연구용
Lapatinib Ditosylate HER2 inhibitor
제품 번호: S1028
화학 구조
분자량: 925.46
바로가기
품질 관리 (Quality Control)
배치:
순도:
99.98%
99.98
세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| HN5 cell line | Proliferation assay | Antiproliferative activity against human HN5 cell line, IC50=0.025 μM | 16483772 | |||
| BT474 cell line | Proliferation assay | Antiproliferative activity against human BT474 cell line, IC50=0.025 μM | 16483772 | |||
| HN5 cell | Growth inhibition assay | Inhibition of HN5 cell growth after 72 hrs, IC50=0.12 μM | 16777410 | |||
| BT474 cell | Growth inhibition assay | Inhibition of BT474 cell growth after 72 hrs, IC50=0.08 μM | 16777410 | |||
| N87 cell | Growth inhibition assay | Inhibition of N87 cell growth after 72 hrs, IC50=0.08 μM | 16777410 | |||
| HFF cell | Growth inhibition assay | Inhibition of HFF cell growth, IC50=9.9 μM | 16777410 | |||
| BT474 | Antiproliferative assay | Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50=0.025μM | 18653333 | |||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50=0.017μM | 19028425 | ||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50=0.029μM | 19888761 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50=0.104μM | 19888761 | ||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50=0.04μM | 20143778 | |||
| SKHEP1 | Antiproliferative assay | Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50=5.3μM | 20143778 | |||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50=5.4μM | 20143778 | |||
| Hep3B2 | Antiproliferative assay | Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50=5.49μM | 20143778 | |||
| HepG2 | Antiproliferative assay | Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50=6.27μM | 20143778 | |||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50=6.6μM | 20143778 | |||
| A431 | Function assay | Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50=0.052μM | 20346655 | |||
| N87 | Function assay | Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50=0.1μM | 20346655 | |||
| MIAPaCa | Function assay | Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50=0.14μM | 20817523 | |||
| MIAPaCa | Function assay | Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50=0.433μM | 20817523 | |||
| SKBR3 | Cytotoxicity assay | Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50=0.002μM | 21080629 | |||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50=0.003μM | 21080629 | |||
| CAL27 | Cytotoxicity assay | Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50=0.007μM | 21080629 | |||
| CAL27 | Function assay | 16 hrs | Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot, IC50<0.032μM | 21080629 | ||
| A431 | Cytotoxicity assay | Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50=0.97μM | 21080629 | |||
| HeLa | Cytotoxicity assay | Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50=5.9μM | 21080629 | |||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50=8.5μM | 21080629 | |||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50=4.35μM | 21570843 | |||
| MDA-MB-468 | Antiproliferative assay | Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50=23.46μM | 21570843 | |||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells by MTT assay, IC50=42.36μM | 21570843 | |||
| BT474 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50=0.025μM | 21887403 | ||
| NCI-N87 | Antiproliferative assay | 3 days | Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining, IC50=0.09μM | 22101132 | ||
| BT474 | Antiproliferative assay | 3 days | Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50=0.1μM | 22101132 | ||
| NCI-N87 | Antitumor assay | 20 mg/kg | 14 days | Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor growth inhibition at 20 mg/kg, po QD for 14 days measured after 19 days | 22101132 | |
| DIFI | Cytotoxicity assay | 4 days | Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=0.235μM | 22169601 | ||
| CAL27 | Cytotoxicity assay | 4 days | Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=0.53μM | 22169601 | ||
| GXF251L | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=1.48μM | 22169601 | ||
| LXFA 629L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=2.87μM | 22169601 | ||
| DU145 | Cytotoxicity assay | 4 days | Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=2.99μM | 22169601 | ||
| OVXF 899L | Cytotoxicity assay | 4 days | Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=3.35μM | 22169601 | ||
| LXFL 529L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=3.51μM | 22169601 | ||
| LNCAP | Cytotoxicity assay | 4 days | Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=3.68μM | 22169601 | ||
| LXFA 526L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.21μM | 22169601 | ||
| UXF 1138L | Cytotoxicity assay | 4 days | Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.4μM | 22169601 | ||
| PC3M | Cytotoxicity assay | 4 days | Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.55μM | 22169601 | ||
| HT-29 | Cytotoxicity assay | 4 days | Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.62μM | 22169601 | ||
| MCF7 | Cytotoxicity assay | 4 days | Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.83μM | 22169601 | ||
| MEXF 1341L | Cytotoxicity assay | 4 days | Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.85μM | 22169601 | ||
| RKO | Cytotoxicity assay | 4 days | Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=5.35μM | 22169601 | ||
| LXFA 289L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=5.79μM | 22169601 | ||
| MAXF 401NL | Cytotoxicity assay | 4 days | Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=5.8μM | 22169601 | ||
| 22Rv1 | Cytotoxicity assay | 4 days | Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=6.06μM | 22169601 | ||
| PAXF 546L | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=6.12μM | 22169601 | ||
| PXF 1118L | Cytotoxicity assay | 4 days | Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=6.86μM | 22169601 | ||
| LIXF 575L | Cytotoxicity assay | 4 days | Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=7.18μM | 22169601 | ||
| RXF 1781L | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=7.67μM | 22169601 | ||
| MDA231 | Cytotoxicity assay | 4 days | Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=7.7μM | 22169601 | ||
| LXFL 1121L | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=7.73μM | 22169601 | ||
| RXF 393NL | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=7.77μM | 22169601 | ||
| PANC1 | Cytotoxicity assay | 4 days | Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=8.12μM | 22169601 | ||
| CXF 269L | Cytotoxicity assay | 4 days | Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=8.36μM | 22169601 | ||
| RXF 486L | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=9.1μM | 22169601 | ||
| Saos2 | Cytotoxicity assay | 4 days | Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=9.38μM | 22169601 | ||
| PXF 1752L | Cytotoxicity assay | 4 days | Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=9.46μM | 22169601 | ||
| PXF 698L | Cytotoxicity assay | 4 days | Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=9.49μM | 22169601 | ||
| BXF T24 | Cytotoxicity assay | 4 days | Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=9.65μM | 22169601 | ||
| MEXF 462NL | Cytotoxicity assay | 4 days | Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=10.13μM | 22169601 | ||
| TE671 | Cytotoxicity assay | 4 days | Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=10.95μM | 22169601 | ||
| PAXF 1657L | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=11.11μM | 22169601 | ||
| MEXF 276L | Cytotoxicity assay | 4 days | Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=11.37μM | 22169601 | ||
| MKN45 | Cytotoxicity assay | 4 days | Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=11.48μM | 22169601 | ||
| BXF 1352L | Cytotoxicity assay | 4 days | Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=11.53μM | 22169601 | ||
| BXF 1218L | Cytotoxicity assay | 4 days | Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=11.77μM | 22169601 | ||
| HCT116 | Cytotoxicity assay | 4 days | Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=13.14μM | 22169601 | ||
| OVCAR3 | Cytotoxicity assay | 4 days | Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=13.44μM | 22169601 | ||
| H460 | Cytotoxicity assay | 4 days | Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=13.46μM | 22169601 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50=2.62μM | 22182581 | ||
| SKOV3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay, IC50=2.99μM | 22182581 | ||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay, IC50=0.029μM | 22372864 | ||
| NCI-N87 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay, IC50=0.036μM | 22372864 | ||
| MDA-MB-175 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-175 cells expressing Src, Ret and low HER-2 after 72 hrs by SRB assay, IC50=0.0444μM | 22372864 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay, IC50=0.104μM | 22372864 | ||
| MDA-MB-453 | Cytotoxicity assay | 72 hrs | Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay, IC50=0.555μM | 22372864 | ||
| MDA-MB-361 | Cytotoxicity assay | 72 hrs | Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay, IC50=1.029μM | 22372864 | ||
| NCI-H1781 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1781 cells expressing HER-2 G776insV_G/C after 72 hrs by SRB assay, IC50=3.047μM | 22372864 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50=2.6μM | 22595177 | ||
| NIH/3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50=4.3μM | 22595177 | ||
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay, IC50=5.05μM | 23927972 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50=15.71μM | 24355130 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50=15.79μM | 24355130 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50=19.22μM | 24355130 | ||
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2delta16 at 10 uM after 2 hrs by Western blotting | 24355130 | |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2 at 10 uM after 2 hrs by Western blotting | 24355130 | |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting | 24355130 | |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of HER2 delta16 mutant autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting | 24355130 | |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting | 24355130 | |
| MCF7 | Function assay | 10 uM | 2 hrs | Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting | 24355130 | |
| 4T1 | Cytotoxicity assay | Cytotoxicity against mouse triple negative 4T1 cells, IC50=0.01037μM | 24890652 | |||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human triple negative MDA-MB-231 cells, IC50=0.02μM | 24890652 | |||
| MDA-MB-435 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-435 cells, IC50=0.0297μM | 24890652 | |||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human ER-positive MCF7 cells, IC50=0.0649μM | 24890652 | |||
| MDA-MB-468 | Cytotoxicity assay | Cytotoxicity against human triple negative MDA-MB-468 cells, IC50=0.0832μM | 24890652 | |||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50=0.011μM | 25151582 | ||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=0.0301μM | 25305330 | ||
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=0.0639μM | 25305330 | ||
| MDA-MB-453 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=0.19μM | 25305330 | ||
| Calu3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=0.23μM | 25305330 | ||
| SKOV3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=0.59μM | 25305330 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=0.6431μM | 25305330 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50=8.468μM | 25305330 | ||
| A431 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER1 phosphorylation (unknown origin) expressed in human A431 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 | |
| BT474 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER2 phosphorylation (unknown origin) expressed in human BT474 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 | |
| A431 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 | |
| A431 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 | |
| BT474 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 | |
| BT474 | Function assay | 0.001 to 10 uM | 2 hrs | Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method | 25305330 | |
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay, GI50=0.93μM | 26475520 | ||
| HeLa | Antiproliferative assay | 12 hrs | Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50=0.12μM | 26652482 | ||
| B16F10 | Antiproliferative assay | 12 hrs | Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50=0.21μM | 26652482 | ||
| HepG2 | Antiproliferative assay | 12 hrs | Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50=0.27μM | 26652482 | ||
| MCF7 | Antiproliferative assay | 12 hrs | Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50=0.47μM | 26652482 | ||
| SKBR3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50=0.49μM | 27187856 | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=6.74μM | 27187856 | ||
| LLC | Antitumor assay | 100 mg/kg | 14 days | Antitumor activity against mouse LLC cells implanted in in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 14 days | 27187856 | |
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay, IC50=0.031μM | 27288180 | ||
| SK-BR-3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50=0.06μM | 27769671 | ||
| BT474 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50=0.1μM | 27769671 | ||
| A431 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50=0.15μM | 27769671 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50=0.51μM | 27769671 | ||
| Calu3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay, IC50=0.1μM | 28092860 | ||
| A431NS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay, IC50=0.6μM | 28092860 | ||
| Bel7402 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50=3.7μM | 28092860 | ||
| SK-BR-3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay, IC50=4.4μM | 28092860 | ||
| COLO205 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay, IC50=4.6μM | 28092860 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=6.2μM | 28092860 | ||
| NCI-H522 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay, IC50=6.4μM | 28092860 | ||
| NCI-H460 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50=8.4μM | 28092860 | ||
| MDA-MB-468 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay, IC50=20μM | 28092860 | ||
| NCI-H522 | Antitumor assay | 100 mg/kg | 28 days | Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ig administered once daily for 28 days relative to control | 28092860 | |
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50=4.8μM | 28238614 | ||
| NCI-H1975 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50=9.08μM | 28238614 | ||
| SW480 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50=12.58μM | 28238614 | ||
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50=14.9μM | 28238614 | ||
| A549 | Function assay | 50 uM | 2 hrs | Inhibition of EGFR phosphorylation at Tyr residue in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method | 28238614 | |
| A549 | Function assay | 50 uM | 2 hrs | Inhibition of EGFR phosphorylation at Y1068 in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method | 28238614 | |
| RAW264.7 | Antileishmanial assay | 96 hrs | Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay, EC50=11μM | 28337329 | ||
| 3T3 | Antitrypanosomal assay | 48 hrs | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay, EC50=13μM | 28337329 | ||
| HEK293 | Function assay | Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50=0.02706μM | 28711703 | |||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=4.8μM | 28711703 | ||
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50=9.08μM | 28711703 | ||
| SW480 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=12.58μM | 28711703 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay, IC50=14.9μM | 28711703 | ||
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50=6.27μM | 29049963 | |||
| BT474 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50=0.2μM | 29089259 | ||
| EOL-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50=0.41μM | 29089259 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50=5.7μM | 29089259 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50=8.1μM | 29089259 | ||
| HCC827 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50=22.3μM | 29089259 | ||
| HEK293 | Function assay | Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50=0.0271μM | 29421573 | |||
| HCC827 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay, IC50=0.6μM | 29421573 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=4.8μM | 29421573 | ||
| SW480 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=12.58μM | 29421573 | ||
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=12.68μM | 29421573 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50=14.9μM | 29421573 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=6.8μM | 29684708 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=10.12μM | 29684708 | ||
| A2780 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50=10.4μM | 29684708 | ||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells over expressing HER2 assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay, IC50=0.17μM | 29902719 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells over expressing EGFR assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay, IC50=1.69μM | 29902719 | ||
| NCI-H1975 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay, IC50=11.46μM | 29902719 | ||
| MDA-MB-361 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-361 cells over expressing HER2 assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay, IC50=13.73μM | 29902719 | ||
| HepG2 | Function assay | Inhibition of EGFR in human HepG2 cells, IC50=0.0271μM | 30096580 | |||
| insect cells | Function assay | 5 mins | Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50=0.03755μM | 30096580 | ||
| Sf21 | Function assay | 5 mins | Inhibition of N-terminal GST-tagged recombinant human EGFR T790M mutant expressed in baculovirus infected Sf21 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50=0.22489μM | 30096580 | ||
| MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay, IC50=5.02μM | 30096580 | ||
| HCT116 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay, IC50=5.92μM | 30096580 | ||
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50=11.71μM | 30096580 | ||
| Caco | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Caco cells after 24 hrs by SRB assay, IC50=12.11μM | 30096580 | ||
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells, TC50=6.3μM | 30344906 | |||
| L929 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=2.05μM | 30508379 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells after 72 hrs by MTT assay, IC50=2.66μM | 30508379 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3.64μM | 30508379 | ||
| A549 | Cytotoxicity assay | 6 uM | 24 hrs | Cytotoxicity against human A549 cells assessed as effect on intracellular ATP levels at 6 uM after 24 hrs by luciferase-luciferin based assay | 30508379 | |
| HN5 | Function assay | 24 hrs | Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis, IC50=0.01μM | 30600149 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.691μM | 30792101 | ||
| MDA231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay, IC50=4.691μM | 30792101 | ||
| SK-MEL-19 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=5μM | 30802730 | ||
| JeKo1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=5μM | 30802730 | ||
| MIAPaCa2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=10μM | 30802730 | ||
| U87MG | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=10μM | 30802730 | ||
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=10μM | 30802730 | ||
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=20μM | 30802730 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=20μM | 30802730 | ||
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=20μM | 30802730 | ||
| T47D | Antiproliferative assay | 72 hrs | Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay, GI50=40μM | 30802730 | ||
| A431 | Function assay | 90 mins | Inhibition of EGFR in human A431 cells assessed as reduction in EGF-stimulated EGFR autophosphorylation preincuabted for 90 mins followed by EGF-stimulation by sandwich-ELISA, IC50=0.021μM | 30973735 | ||
| UCH1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human UCH1 cells measured after 72 hrs by alamar blue assay, IC50=3.2μM | 30973735 | ||
| WS1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human WS1 cells measured after 72 hrs by alamar blue assay, IC50=13μM | 30973735 | ||
| UMCHOR1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human UMCHOR1 cells measured after 72 hrs by alamar blue assay, IC50=25μM | 30973735 | ||
| CH22 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CH22 cells measured after 72 hrs by alamar blue assay, IC50=25μM | 30973735 | ||
| UCH7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human UCH7 cells measured after 72 hrs by alamar blue assay, IC50=26μM | 30973735 | ||
| UCH12 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human UCH12 cells measured after 72 hrs by alamar blue assay, IC50=33μM | 30973735 | ||
| A549 | Function assay | 86 mM/kg | 27 days | Drug concentration in NOD/SCID mouse blood xenografted with human A549 cells overexpressing EGFR at 86 micromol/kg, po administered once daily for 27 days and measured at day 27 at 2 hrs after last administered dose by LC-MS/MS analysis, Ct=2.81μM | 31125894 | |
| HCC1954 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5μM | 31125894 | ||
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=9μM | 31125894 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=11μM | 31125894 | ||
| Sf9 | Function assay | 1 to 10 uM | 60 mins | Inhibition of human recombinant GST-tagged EGFR (catalytic domain 695 to end residues) autophosphorylation expressed in baculovirus infected Sf9 cells using poly( Glu,Tyr) 4:1 as substrate at 1 to 10 uM incubated for 60 mins by ELISA | 31125894 | |
| HCC1954 | Function assay | 0.02 to 2 uM | 1 hr | Inhibition of HER2 autophosphorylation in human HCC1954 cells overexpressing HER2 at 0.02 to 2 uM incubated for 1 hr by Western blot analysis | 31125894 | |
| HCC827 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay, IC50=0.6μM | 31202990 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay, IC50=4.8μM | 31202990 | ||
| SW480 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay, IC50=12.58μM | 31202990 | ||
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay, IC50=12.68μM | 31202990 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay, IC50=14.9μM | 31202990 | ||
| A549 | Function assay | 15 uM | 48 hrs | Inhibition of cell migration in CM-dil-labelled human A549 cells xenografted in 48 hrs post-fertilization zebrafish embryos at 15 uM incubated for 48 hrs by confocal microscopic method | 31202990 | |
| WS1 | Cytotoxicity assay | Cytotoxicity in human WS1 cells assessed as reduction in cell viability incubated fro 48 hrs by alamar blue dye based assay, IC50=13μM | 31378571 | |||
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=9.76μM | 31546197 | ||
| SUM159 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=9.76μM | 31546197 | ||
| KG1a | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=9.76μM | 31546197 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay, IC50=6.8μM | 31655429 | ||
| A2780 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay, IC50=10.4μM | 31655429 | ||
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay, IC50=12.67μM | 31655429 | ||
| MRC5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay, IC50=13.66μM | 31655429 | ||
| NCI-H1648 cell | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.02544 μM | SANGER | |||
| NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=3.54501 μM | SANGER | |||
| NTERA-S-cl-D1 cell | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=6.26561 μM | SANGER | |||
| OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=0.0574 μM | SANGER | |||
| OS-RC-2 cell | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=1.99199 μM | SANGER | |||
| OVCAR-4 cell | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=9.11675 μM | SANGER | |||
| RL95-2 cell | Growth inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=3.1567 μM | SANGER | |||
| SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=5.39245 μM | SANGER | |||
| SW962 cell | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay, IC50=5.39245 μM | SANGER | |||
| TE-1 cell | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50=5.02159 μM | SANGER | |||
| A253 cell | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay, IC50=2.0483 μM | SANGER | |||
| A388 cell | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50=2.0483 μM | SANGER | |||
| BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.97335 μM | SANGER | |||
| TE-12 cell | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50=0.72258 μM | SANGER | |||
| TE-5 cell | Growth inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay, IC50=0.24654 μM | SANGER | |||
| TE-6 cell | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50=0.49057 μM | SANGER | |||
| TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=4.0373 μM | SANGER | |||
| TE-9 cell | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay, IC50=1.55201 μM | SANGER | |||
| TK10 cell | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay, IC50=4.16522 μM | SANGER | |||
| DSH1 cell | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50=0.09396 μM | SANGER | |||
| ECC12 cell | Growth inhibition assay | Inhibition of human ECC12 cell growth in a cell viability assay, IC50=0.09231 μM | SANGER | |||
| EKVX cell | Growth inhibition assay | Inhibition of human EKVX cell growth in a cell viability assay, IC50=0.44874 μM | SANGER | |||
| HCC2218 cell | Growth inhibition assay | Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=0.05326 μM | SANGER | |||
| LB2241-RCC cell | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=1.15403 μM | SANGER | |||
| LB996-RCC cell | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=1.36228 μM | SANGER | |||
| LC-1F cell | Growth inhibition assay | Inhibition of human LC-1F cell growth in a cell viability assay, IC50=1.38244 μM | SANGER | |||
| LS-513 cell | Growth inhibition assay | Inhibition of human LS-513 cell growth in a cell viability assay, IC50=3.40041 μM | SANGER | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)
| 분자량 | 925.46 | 화학식 | C29H26ClFN4O4S.2C7H8O3S |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 388082-77-7 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | GW-572016 Ditosylate | Smiles | CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl | ||
용해도 (Solubility)
|
In vitro |
DMSO
: 186 mg/mL
(200.98 mM)
Water : Insoluble Ethanol : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
|||||
생체 내 제형 계산기 (투명한 용액)
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
mg/kg
g
μL
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
작용 메커니즘 (Mechanism of Action)
| Targets/IC50/Ki |
ErbB2
(Cell-free assay) 9.2 nM
EGFR
(Cell-free assay) 10.8 nM
ErbB4
(Cell-free assay) 367 nM
|
|---|---|
| 시험관 내(In vitro) |
Lapatinib Ditosylate weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. This compound significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, it inhibits the growth of both EGFR- and ErbB2-overexpressing cells. It displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. This chemical potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation.
|
| 키나아제 분석 |
In vitro kinase 분석
|
|
효소 활성 억제에 대한 IC50 값은 펩타이드 기질의 인산화 억제를 측정하여 생성됩니다. EGFR 및 ErbB2의 세포 내 키나아제 도메인은 바큘로바이러스 발현 시스템에서 정제됩니다. EGFR 및 ErbB2 반응은 최종 부피 45 μL의 96웰 폴리스티렌 라운드 바텀 플레이트에서 수행됩니다. 반응 혼합물에는 50 mM 4-모르폴린프로판술폰산(pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi [γ33P] ATP/반응, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM 디티오트레이톨, 그리고 10 μM부터 시작하는 이 화합물의 연속 희석액이 포함된 DMSO 1 μL가 포함됩니다. 반응은 표시된 정제된 type-1 수용체 세포 내 도메인을 첨가하여 시작됩니다. 첨가된 효소의 양은 반응당 1 pmol(20 nM)입니다. 반응은 23°C에서 10분 후 물에 0.5% 인산을 녹인 용액 45 μL를 첨가하여 종료됩니다. 종료된 반응 혼합물(75 μL)은 포스포셀룰로오스 필터 플레이트로 옮겨집니다. 플레이트를 여과하고 0.5% 인산 200 μL로 3회 세척합니다. 신틸레이션 칵테일(50 μL)을 각 웰에 첨가하고, Packard Topcount에서 계수하여 분석을 정량화합니다. IC50 값은 10점 용량-반응 곡선으로부터 생성됩니다.
|
|
| 생체 내(In vivo) |
Oral administration of Lapatinib Ditosylate (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner.
|
참조 |
적용 분야 (Applications)
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | pEGFR / EGFR / p-mTOR / mTOR / PARP / c-PARP p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk |
|
28938602 |
| Growth inhibition assay | Cell viability |
|
24947784 |
임상시험 정보 (Clinical Trial Information)
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT00455039 | Withdrawn | Breast Cancer |
University of New Mexico |
July 31 2023 | Phase 1|Phase 2 |
| NCT04608409 | Active not recruiting | Ovarian Cancer |
Frederick R. Ueland M.D.|National Cancer Institute (NCI)|University of Kentucky |
March 17 2021 | Phase 1 |
| NCT03075995 | Unknown status | Breast Cancer |
Sun Yat-sen University |
April 12 2017 | Not Applicable |
| NCT02338245 | Completed | Metastatic Breast Cancer |
ASLAN Pharmaceuticals |
December 29 2014 | Phase 2 |
| NCT02294786 | Terminated | Cancer |
Novartis Pharmaceuticals|Novartis |
December 17 2014 | Phase 2 |
| NCT02158507 | Active not recruiting | Metastatic Triple Negative Breast Cancer |
University of Alabama at Birmingham|Breast Cancer Research Foundation of Alabama|GlaxoSmithKline|AbbVie |
September 2014 | Not Applicable |
자주 묻는 질문 (Frequently Asked Questions)
질문 1:
If I need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution?
답변:
It can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution.
제품은 연구용으로만 사용됩니다. 인체에는 사용하지 마십시오. 환자에게 판매하지 않습니다.
©Copyright 2013 Selleck Chemicals. All Rights Reserved.