연구용
제품 번호S1021
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| M07ep210 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.00007 μM | 17956080 | |
| K562 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.001 μM | 17956080 | |
| M07e | Growth Inhibition Assay | 72 h | DMSO | IC50=0.0012 μM | 17956080 | |
| ALL3 | Cytotoxic Assay | 0.1μM | 72 h | DMSO | IC50=0.0004 μM | 19889540 |
| CML | Growth Inhibition Assay | 20 min | DMSO | IC50=0.001 μM | 19219016 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | IC50=6.589 μM | 23088644 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant with IC50 of 0.00083μM | 23088644 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl with IC50 of 0.0045μM | 23088644 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant with IC50 of 1.714μM | 23088644 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth Inhibition with IC50 of 0.0009μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth Inhibition with IC50 of 0.0032μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth Inhibition with IC50 of 0.0051μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth Inhibition with IC50 of 0.008μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth Inhibition with IC50 of 0.0013μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth Inhibition with IC50 of 0.0019μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth Inhibition with IC50 of 0.0023μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth Inhibition with IC50 of 3.6μM | 23301703 | |
| BA/F3 | Growth Inhibition Assay | 72 h | DMSO | Induces cytotoxicity against mouse BA/F3 cells assessed as growth Inhibition with IC50 of 2.5μM | 23301703 | |
| T cell | Growth Inhibition Assay | 72 h | DMSO | Inhibits anti CD3- and anti CD28-induced T cell proliferation with IC50 of 0.003μM | 17154512 | |
| WiDr | Growth Inhibition Assay | 72 h | DMSO | IC50=0.052 μM | 15615512 | |
| PC3 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.0094 μM | 15615512 | |
| MDA-MB-231 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.012 μM | 15615512 | |
| Hs578T | Cytotoxic Assay | 72 h | DMSO | GI50=0.03 μM | 24015327 | |
| HMEC | Cytotoxic Assay | 72 h | DMSO | GI50=1.8 μM | 24015327 | |
| DU145 | Cytotoxic Assay | 72 h | DMSO | GI50=0.16 μM | 24015327 | |
| U251 | Cytotoxic Assay | 72 h | DMSO | GI50=2.81 μM | 24015327 | |
| NCI60 | Cytotoxic Assay | 72 h | DMSO | GI50=5.7 μM | 24015327 | |
| MALME-3M | Cytotoxic Assay | 72 h | DMSO | GI50=6.61 μM | 24015327 | |
| KM12 | Cytotoxic Assay | 72 h | DMSO | GI50=7.44 μM | 24015327 | |
| SW620 | Cytotoxic Assay | 72 h | DMSO | GI50=8.43 μM | 24015327 | |
| RXF 393NL | Cytotoxic Assay | 4 days | DMSO | IC50=0.0217 μM | 23253074 | |
| LXFA 983L | Cytotoxic Assay | 4 days | DMSO | IC50=0.0565 μM | 23253074 | |
| PRXF DU145 | Cytotoxic Assay | 4 days | DMSO | IC50=0.0623 μM | 23253074 | |
| PAXF 1657L | Cytotoxic Assay | 4 days | DMSO | IC50=0.121 μM | 23253074 | |
| CXF 1103L | Cytotoxic Assay | 4 days | DMSO | IC50=4.36 μM | 23253074 | |
| GXF251L | Cytotoxic Assay | 4 days | DMSO | IC50=2.25 μM | 23253074 | |
| NCI-H23 | Growth Inhibition Assay | 72 h | DMSO | IC50=2.27 μM | 23521020 | |
| HCT116 | Growth Inhibition Assay | 72 h | DMSO | IC50=2.3 μM | 23521020 | |
| MCF7 | Growth Inhibition Assay | 72 h | DMSO | IC50=2.57 μM | 23521020 | |
| NCI-H460 | Growth Inhibition Assay | 72 h | DMSO | IC50=8.99 μM | 23521020 | |
| DLD1 | Growth Inhibition Assay | 72 h | DMSO | IC50=4.6 μM | 23567960 | |
| NCI-H661 | Growth Inhibition Assay | 72 h | DMSO | IC50=7.8 μM | 23567960 | |
| A549 | Growth Inhibition Assay | 72 h | DMSO | IC50=8.2 μM | 23567960 | |
| U937 | Growth Inhibition Assay | 72 h | DMSO | IC50=12.2 μM | 23567960 | |
| HEK293 | Function Assay | 10 μM | DMSO | Induces binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells with IC50 of 0.063μM | 22770610 | |
| HUVEC | Growth Inhibition Assay | 0.15 μM | 72 h | DMSO | Induces antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as Inhibition of cell growth at 0.15 uM | 22853993 |
| HUVEC | Function Assay | 15 μM | 72 h | DMSO | Induces antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as Inhibition of network formation at 1.8 to 15 uM | 22853993 |
| Plasmodium falciparum | Function Assay | 10 μM | 15 min | DMSO | Inhibits Plasmodium falciparum proliferation by inhibiting the Function of PfCDPK1 protein with IC50 of 1.17μM | 24550330 |
| PC3 | Function Assay | 0.1 μM | 5 h | DMSO | Inhibits human PC3 cell adhesion at 100 nM | 19462975 |
| DU145 | Function Assay | 0.1 μM | 5 h | DMSO | Inhibits human DU145 cell adhesion at 100 nM | 19462975 |
| PC3 | Kinase Assay | 0.1 μM | 5 h | DMSO | Inhibits cSrc in human PC3 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM | 19462975 |
| DU145 | Kinase Assay | 0.1 μM | 5 h | DMSO | Inhibits cSrc in human DU145 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM | 19462975 |
| PC3 | Kinase Assay | 0.1 μM | 5 h | DMSO | Inhibits cSrc in human PC3 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM | 19462975 |
| DU145 | Kinase Assay | 0.1 μM | 5 h | DMSO | Inhibits cSrc in human DU145 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM | 19462975 |
| Huh7 | Antiviral Assay | 2.5 μM | 4 days | DMSO | Inhibits viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM | 17360676 |
| C6/36 | Antiviral Assay | 2.5 μM | 4 days | DMSO | Inhibits viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM | 17360676 |
| U937 | Function Assay | 1 μM | 1 h | DMSO | Reduces basal TNFalpha release in human U937 cells | 17684099 |
| U937 | Function Assay | 1 μM | 1 h | DMSO | Reduces LPS-induced TNFalpha release in human U937 cells | 17684099 |
| murine mast cell | Function Assay | 1 μM | 24 h | DMSO | Inhibits antigen-induced IL6 secretion in IgE primed mouse mast cells at 1 uM | 17684099 |
| FDC-P1 | Function assay | 48 hrs | IC50 = 0.0074 μM | 20156689 | ||
| K562 | Cytotoxicity assay | 72 hrs | IC50 = 12.83 μM | 22217877 | ||
| U937 | Cytotoxicity assay | 72 hrs | IC50 = 13.63 μM | 22217877 | ||
| Sf21 | Function assay | 5 mins | IC50 = 10 μM | 22961681 | ||
| Ba/F3 | Function assay | 1 hr | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis | 23600806 | ||
| Ba/F3 | Function assay | 1 hr | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis | 23600806 | ||
| Ba/F3 | Function assay | 1 hr | Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis | 23600806 | ||
| Sf9 | Function assay | 15 to 20 mins | IC50 = 13.1 μM | 23956101 | ||
| Sf9 | Function assay | 20 mins | IC50 = 27.3 μM | 23956101 | ||
| HMC-1.2 | Antiproliferative assay | IC50 = 0.82 μM | 25004409 | |||
| RXF 393NL | Antiproliferative assay | 4 days | GI50 = 0.0217 μM | 25076195 | ||
| LXFA 983L | Antiproliferative assay | 4 days | GI50 = 0.0565 μM | 25076195 | ||
| PRXF DU145 | Antiproliferative assay | 4 days | GI50 = 0.0623 μM | 25076195 | ||
| PAXF 1657L | Antiproliferative assay | 4 days | GI50 = 0.121 μM | 25076195 | ||
| GXF251L | Antiproliferative assay | 4 days | GI50 = 2.25 μM | 25076195 | ||
| CXF 1103L | Antiproliferative assay | 4 days | GI50 = 4.36 μM | 25076195 | ||
| SH-SY5Y | Apoptosis assay | 0.1 uM | 24 hrs | Induction of apoptosis in human SH-SY5Y cells assessed as accumulation of hypodiploid cells at 0.1 uM after 24 hrs by propidium iodide staining-based cytofluorimetry | 25469771 | |
| ECRF24 | Cytotoxicity assay | 72 hrs | IC50 = 5.7 μM | 25815152 | ||
| A2780 | Cytotoxicity assay | 72 hrs | IC50 = 8.7 μM | 25815152 | ||
| HEK293 | Cytotoxicity assay | 72 hrs | IC50 = 14.3 μM | 25815152 | ||
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | IC50 = 0.178 μM | 25835317 | ||
| MDA-MB-231 | Antiinvasive assay | 0.1 uM | 24 hrs | Antiinvasive activity against human MDA-MB-231 cells at 0.1 uM after 24 hrs by transwell assay | 25835317 | |
| MDA-MB-231 | Cell cycle assay | 0.3 uM | 24 to 48 hrs | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 0.3 uM after 24 to 48 hrs by flow cytometric analysis | 25835317 | |
| MDA-MB-231 | Function assay | >0.03 uM | 20 hrs | Inhibition of Src in human MDA-MB-231 cells assessed as reduction of FAK phosphorylation at >0.03 uM after 20 hrs by Western blot analysis | 25835317 | |
| MDA-MB-231 | Antimigratory assay | 0.03 to 0.3 uM | 20 hrs | Antimigratory activity against human MDA-MB-231 cells at 0.03 to 0.3 uM after 20 hrs by wound healing assay | 25835317 | |
| MDA-MB-231 | Function assay | 0.001 to 1 uM | 20 hrs | Inhibition of Src phosphorylation in human MDA-MB-231 cells at 0.001 to 1 uM after 20 hrs by Western blot analysis | 25835317 | |
| MDA-MB-231 | Antiproliferative assay | >0.01 uM | 12 days | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of colony formation at >0.01 uM after 12 days by crystal violet staining-based assay | 25835317 | |
| MDA-MB-231 | Antitumor assay | 40 mg/kg/day | 18 days | Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 40 mg/kg/day administered for 18 days measured every 3 days during compound dosing | 25835317 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | IC50 = 1.12 μM | 25899332 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | IC50 = 8.05 μM | 25899332 | ||
| HCC366 | Antiproliferative assay | 72 hrs | IC50 = 0.029 μM | 26191369 | ||
| NCI-H2286 | Antiproliferative assay | 72 hrs | IC50 = 0.032 μM | 26191369 | ||
| K562 | Antiproliferative assay | 72 hrs | IC50 = 0.001 μM | 26195136 | ||
| K562 | Cytotoxicity assay | IC50 = 0.08 μM | 26264503 | |||
| IR-K562 | Cytotoxicity assay | IC50 = 1.9 μM | 26264503 | |||
| THP1 | Cytotoxicity assay | IC50 = 6 μM | 26264503 | |||
| HEK293 | Cytotoxicity assay | CC50 = 16 μM | 26264503 | |||
| K562 | Cytotoxicity assay | 48 hrs | IC50 = 0.45 μM | 26451772 | ||
| K562 | Antiproliferative assay | 72 hrs | GI50 = 0.0003 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.0003 μM | 26789553 | ||
| KU812 | Antiproliferative assay | 72 hrs | GI50 = 0.0003 μM | 26789553 | ||
| MEG01 | Antiproliferative assay | 72 hrs | GI50 = 0.0003 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.001 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.001 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.001 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.003 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.003 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.003 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.003 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.004 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.004 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.005 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.008 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.008 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.01 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.014 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.014 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.017 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 0.039 μM | 26789553 | ||
| CHL | Antiproliferative assay | 72 hrs | GI50 = 0.27 μM | 26789553 | ||
| MOLM14 | Antiproliferative assay | 72 hrs | GI50 = 2.3 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 3 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 3 μM | 26789553 | ||
| MV4-11 | Antiproliferative assay | 72 hrs | GI50 = 3.6 μM | 26789553 | ||
| HEL | Antiproliferative assay | 72 hrs | GI50 = 5.3 μM | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | GI50 = 9.94 μM | 26789553 | ||
| KU812 | Function assay | 0.1 uM | 1 hr | Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 26789553 | |
| KU812 | Function assay | 0.1 uM | 1 hr | Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 26789553 | |
| MEG01 | Function assay | 0.1 uM | 1 hr | Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 26789553 | |
| MEG01 | Function assay | 0.1 uM | 1 hr | Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 26789553 | |
| K562 | Function assay | 0.1 uM | 1 hr | Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 26789553 | |
| K562 | Function assay | 0.1 uM | 1 hr | Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 26789553 | |
| K562 | Cytotoxicity assay | 72 hrs | IC50 = 0.00025 μM | 26814890 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | IC50 = 0.09 μM | 26814890 | ||
| BAF3 | Function assay | 72 hrs | EC50 = 0.00004 μM | 27010810 | ||
| BAF3 | Function assay | 72 hrs | EC50 = 0.00004 μM | 27010810 | ||
| BxPC3 | Antiproliferative assay | 72 hrs | EC50 = 0.033 μM | 27010810 | ||
| MDA-MB-231 | Antiproliferative assay | 72 hrs | EC50 = 0.044 μM | 27010810 | ||
| Caki2 | Antiproliferative assay | 72 hrs | EC50 = 0.055 μM | 27010810 | ||
| NCI-H1975 | Antiproliferative assay | 72 hrs | EC50 = 0.173 μM | 27010810 | ||
| PC3 | Antiproliferative assay | 72 hrs | EC50 = 0.232 μM | 27010810 | ||
| insect | Function assay | 20 mins | IC50 = 0.0005 μM | 27115835 | ||
| MDA-MB-231 | Antiproliferative assay | 5 days | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay | 27115835 | ||
| MDA-MB-231 | Function assay | 3 to 100 nM | 1.5 hrs | Inhibition of SRC phosphorylation at tyrosine 416 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis | 27115835 | |
| MDA-MB-231 | Function assay | 3 to 100 nM | 1.5 hrs | Inhibition of FAK phosphorylation at tyrosine 861 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis | 27115835 | |
| MDA-MB-231 | Antimigratory assay | 10 nM | 6 hrs | Antimigratory activity in human MDA-MB-231 cells assessed as reduction in cell motility at 10 nM at 6 hrs by microscopy based scratch-wound cell migration assay | 27115835 | |
| MCF7 | Antiproliferative assay | 0.03 to 300 uM | 5 days | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability at 0.03 to 300 uM after 5 days by PrestoBlue assay | 27115835 | |
| HCT116 | Cytotoxicity assay | 96 hrs | IC50 = 5.23 μM | 27155464 | ||
| A549 | Cytotoxicity assay | 96 hrs | IC50 = 8.37 μM | 27155464 | ||
| U937 | Cytotoxicity assay | 96 hrs | IC50 = 10.23 μM | 27155464 | ||
| K562 | Cytotoxicity assay | 96 hrs | IC50 = 11.95 μM | 27155464 | ||
| K562 | Cytotoxicity assay | CC50 = 0.25 μM | 27474918 | |||
| K562 | Antiproliferative assay | GI50 = 0.001 μM | 28435526 | |||
| K562 | Function assay | IC50 = 0.000069 μM | 29395973 | |||
| HL60 | Function assay | IC50 = 0.00011 μM | 29395973 | |||
| KG1a | Function assay | IC50 = 8.98 μM | 29395973 | |||
| B16-BL6 | Function assay | 8.13 uM | 24 to 48 hrs | Inhibition of cell migration of mouse B16-BL6 cells at 8.13 uM incubated for 24 to 48 hrs by cell wound scratch assay | 29395973 | |
| MCF7 | Function assay | 7.5 uM | 10 days | Inhibition of colony formation in human MCF7 cells at 7.5 uM incubated for 10 days by crystal violet staining based plate cloning test | 29395973 | |
| 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 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY 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 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 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 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | |||
| HEK293 | Function assay | 1 hr | Ki = 0.0005 μM | 29941193 | ||
| HEK293 | Function assay | 1 hr | IC50 = 0.006 μM | 29941193 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00021 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00025 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00029 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.0003 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00033 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00042 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00077 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00098 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 0.00144 μM | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | GI50 = 2.562 μM | 30137981 | ||
| Vero | qHTS assay | Vero cells viability qHTS for Zika virus inhibitors | 33229545 | |||
| HepG2 | qHTS assay | HepG2 cells viability qHTS for Zika virus inhibitors | 33229545 | |||
| BV-173 | Growth Inhibition Assay | IC50=0.000000109 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=0.000000266 μM | SANGER | |||
| BL-70 | Growth Inhibition Assay | IC50=0.000000822 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.00000108 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.00000321 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.0000098 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.0000131 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=0.0000404 μM | SANGER | |||
| TE-15 | Growth Inhibition Assay | IC50=0.00589 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.00613 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=0.0063 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.00989 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=0.00991 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=0.01115 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=0.01174 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=0.01491 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=0.01576 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=0.01719 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.01834 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=0.01861 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=0.01942 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.02011 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=0.0203 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=0.02157 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=0.02357 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=0.02586 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=0.0273 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=0.02832 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=0.02927 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=0.03003 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=0.03119 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=0.03193 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=0.03487 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.03548 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.03902 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=0.03956 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=0.04049 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=0.04161 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=0.04435 μM | SANGER | |||
| PSN1 | Growth Inhibition Assay | IC50=0.04474 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=0.04609 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=0.04724 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.04761 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=0.05095 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=0.05437 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=0.06118 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=0.06164 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=0.06357 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=0.07284 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=0.07858 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=0.08227 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=0.08308 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=0.08362 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=0.08552 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=0.0949 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=0.09656 μM | SANGER | |||
| RL95-2 | Growth Inhibition Assay | IC50=0.1038 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=0.1054 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.11028 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=0.11292 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=0.11317 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=0.1141 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=0.11606 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.11883 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=0.12213 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.12283 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=0.1345 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=0.14032 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=0.14064 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=0.14162 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=0.14436 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=0.15458 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=0.16489 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=0.16666 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=0.17404 μM | SANGER | |||
| PF-382 | Growth Inhibition Assay | IC50=0.17678 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=0.18413 μM | SANGER | |||
| NALM-6 | Growth Inhibition Assay | IC50=0.19295 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=0.19531 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=0.19987 μM | SANGER | |||
| CP67-MEL | Growth Inhibition Assay | IC50=0.20488 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=0.24001 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=0.26439 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=0.28537 μM | SANGER | |||
| BL-41 | Growth Inhibition Assay | IC50=0.29123 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=0.3142 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=0.31503 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=0.31931 μM | SANGER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.33997 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=0.3498 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=0.3541 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=0.36224 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.37433 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=0.38599 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=0.42951 μM | SANGER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=0.47911 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=0.4911 μM | SANGER | |||
| BOKU | Growth Inhibition Assay | IC50=0.49133 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=0.50228 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=0.50302 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=0.52966 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=0.53609 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=0.6276 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.70629 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=0.74469 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=0.76178 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=0.78165 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=0.82508 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=0.87532 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=0.98452 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=1.03043 μM | SANGER | |||
| OCUB-M | Growth Inhibition Assay | IC50=1.04412 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=1.05145 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=1.21226 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=1.23376 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=1.24412 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=1.30589 μM | SANGER | |||
| NCI-H1838 | Growth Inhibition Assay | IC50=1.30733 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=1.30859 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=1.3622 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=1.39827 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=1.40992 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=1.56714 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=1.57984 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=1.73466 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=1.79139 μM | SANGER | |||
| CAN | Growth Inhibition Assay | IC50=1.82252 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=2.16693 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=2.36284 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=2.57551 μM | SANGER | |||
| NCCIT | Growth Inhibition Assay | IC50=2.86616 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=2.87552 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=3.05741 μM | SANGER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=3.11886 μM | SANGER | |||
| ARH-77 | Growth Inhibition Assay | IC50=3.46915 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=3.63847 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=3.73246 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=4.27685 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=4.36454 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=4.49954 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=4.60845 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=5.86154 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=6.12519 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=6.48558 μM | SANGER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=7.27067 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=7.51671 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=7.54782 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=7.65787 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=8.21652 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=8.27066 μM | SANGER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=8.56128 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=8.72805 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=8.79307 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=8.89155 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=8.96529 μM | SANGER | |||
| SKM-1 | Growth Inhibition Assay | IC50=9.01734 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=9.02012 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=9.02493 μM | SANGER | |||
| EVSA-T | Growth Inhibition Assay | IC50=9.27793 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=9.35546 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=9.92259 μM | SANGER | |||
| EHEB | Growth Inhibition Assay | IC50=10.0656 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=10.4776 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=10.7938 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=11.2828 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=12.1138 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=12.4445 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=12.9198 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=12.9283 μM | SANGER | |||
| Raji | Growth Inhibition Assay | IC50=13.7497 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=13.8557 μM | SANGER | |||
| DMS-153 | Growth Inhibition Assay | IC50=14.0028 μM | SANGER | |||
| L-540 | Growth Inhibition Assay | IC50=15.0672 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=15.1979 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=17.4454 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=19.3973 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=19.4877 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=19.7543 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=20.2733 μM | SANGER | |||
| REH | Growth Inhibition Assay | IC50=20.6357 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=23.146 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=24.5551 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=24.7754 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=26.6753 μM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=27.1422 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=27.3245 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=28.1628 μM | SANGER | |||
| BC-1 | Growth Inhibition Assay | IC50=28.651 μM | SANGER | |||
| NCI-H64 | Growth Inhibition Assay | IC50=29.6253 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=29.6292 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=30.766 μM | SANGER | |||
| GAK | Growth Inhibition Assay | IC50=31.2686 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=32.1252 μM | SANGER | |||
| HCC1599 | Growth Inhibition Assay | IC50=32.3325 μM | SANGER | |||
| EB-3 | Growth Inhibition Assay | IC50=34.3117 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=35.8052 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=36.1943 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=37.2338 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=37.9946 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=38.1009 μM | SANGER | |||
| COR-L279 | Growth Inhibition Assay | IC50=40.2851 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=41.9086 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=42.0163 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=43.0818 μM | SANGER | |||
| NCI-H2107 | Growth Inhibition Assay | IC50=43.4846 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=44.336 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=46.2258 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=48.4748 μM | SANGER | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 488.01 | 화학식 | C22H26ClN7O2S |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 302962-49-8 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | BMS-354825 | Smiles | CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO | ||
|
In vitro |
DMSO
: 98 mg/mL
(200.81 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
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.
| Targets/IC50/Ki |
LCK
Abl
(Cell-free assay) 0.6 nM
Src
(Cell-free assay) 0.8 nM
c-Kit (D816V)
(Cell-free assay) 37 nM
c-Kit (wt)
(Cell-free assay) 79 nM
|
|---|---|
| 시험관 내(In vitro) |
Dasatinib은 T315I를 제외하고 야생형 Bcr-Abl 및 Bcr-Abl 돌연변이를 발현하는 Ba/F3 세포의 증식을 억제하는 데 더 효과적입니다. 이 화합물은 2-log(약 325배) 증가된 효능을 가지고 있습니다. 좁은 범위에서 야생형 Abl 키나아제 및 T315I를 제외한 모든 돌연변이를 강력하게 억제합니다. 이 약물은 야생형 및 돌연변이 Abl 키나아제 도메인을 직접 표적으로 하고 농도 의존적으로 자가인산화 및 기질 인산화를 억제합니다. 야생형 Bcr-Abl을 발현하는 세포에 대해 325배 더 큰 효능을 나타냅니다. TgE 골수 세포 콜로니의 비율은 미처리 웰의 100%에서 이 화합물 처리 웰의 4.12%로 감소합니다. 이 화학 물질의 존재 하에서 WT 및 TgE 골수 세포에 의해 형성된 콜로니 비율의 차이는 통계적으로 유의합니다. LMP2A의 발현은 B 림프구 생존 및 증식을 촉진할 수 있으며, 이는 이 약물을 통해 Lyn 및/또는 c-Abl 키나아제를 표적으로 함으로써 억제될 수 있습니다. 이 치료는 Src 신호 전달을 억제하고 성장을 감소시키며 특정 갑상선암 세포 하위 집합에서 세포 주기 정지 및 apoptosis를 유도합니다. 이 화합물 (0.019 μM ~ 1.25 μM)의 용량을 3일 동안 증가시켜 처리하면 C643, TPC1, BCPAP 및 SW1736 세포주의 성장을 낮은 나노몰 농도에서 약 50% 억제하지만, K1 세포주의 성장을 억제하려면 더 높은 농도가 필요합니다. 10 nM 또는 50 nM의 이 화학 물질로 처리하면 BCPAP, SW1736 및 K1 세포 중에서 G1 개체군 세포가 9-22% 증가하고, S기 세포 비율이 7-18% 감소합니다. |
| 키나아제 분석 |
키나아제 자가인산화 분석
|
|
야생형 및 돌연변이 글루타티온 S-트랜스퍼라제(GST)-Abl 융합 단백질(c-Abl 아미노산 220-498)을 사용하는 키나아제 분석을 수행합니다. GST-Abl 융합 단백질은 사용 전에 글루타티온-세파로스 비드에서 방출됩니다. ATP 농도는 5 μM입니다. 키나아제 자가인산화 및 시험관 내 펩타이드 기질 인산화 분석에 사용하기 직전에 GST-Abl 키나아제 도메인 융합 단백질은 LAR 티로신 포스파타제로 처리됩니다. 30 °C에서 1시간 배양 후, LAR 포스파타제는 바나듐산 나트륨(1 mM)을 첨가하여 비활성화됩니다. 미처리 GST-Abl 키나아제와 탈인산화된 GST-Abl 키나아제를 비교하는 면역블롯 분석은 티로신 잔기의 완전한 (>95%) 탈인산화를 확인하기 위해 포스포티로신 특이 항체 4G10을 사용하여 일상적으로 수행되며, GST-Abl 키나아제의 동등한 로딩을 확인하기 위해 c-Abl 항체 CST 2862를 사용합니다. Dasatinib 농도 범위는 T315I 돌연변이에 대해 1,000 nM로 확장됩니다. 이 동일한 억제제 농도는 시험관 내 펩타이드 기질 인산화 분석에 사용됩니다. 세 가지 억제제는 GST-Src 키나아제 및 GST-Lyn 키나아제에 대해 동일한 농도 범위에서 테스트됩니다.
|
|
| 생체 내(In vivo) |
Dasatinib은 LMP2A/MYC 이중 형질전환 마우스에서 비장비대를 역전시킵니다. 이 화합물은 LMP2A를 발현하는 골수 B 세포의 콜로니 형성을 특이적으로 방지하고 TgE 마우스에서 비장 크기를 감소시켰습니다. 이 화합물로 처리된 Tg6/λ-MYC 마우스의 비장 질량은 대조군에 비해 유의하게 감소했습니다. 이는 LMP2A/MYC 이중 형질전환 마우스의 림프절 비대를 억제합니다. 이 화학 물질은 LMP2A/MYC 이중 형질전환 마우스의 종양 세포를 이식한 Rag1KO 마우스에서 비장비대를 역전시킵니다. 이 치료는 LMP2A를 발현하는 B 림프구 종양에서 Lyn 인산화를 억제합니다. |
참조 |
|
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 p-FAK / p-STAT3 cleaved caspase 3 |
|
23049975 |
| Growth inhibition assay | IC50 |
|
23721490 |
| Immunofluorescence | SRC / Met F-actin / Actinin-4 / Paxillin α-tubulin |
|
26517812 |
| ELISA | TNF-α E-selectin VCAM-1 |
|
17684099 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT05527418 | Recruiting | Recent HIV-1 Infection |
Eva Bonfill|Institut d''Investigacions Biomèdiques August Pi i Sunyer |
January 26 2024 | Phase 2 |
| NCT05993949 | Recruiting | Lymphoblastic Leukemia |
Stanford University|Kite Pharma |
October 2 2023 | Phase 1 |
| NCT05780073 | Recruiting | HIV Infection Primary |
Fundació Institut Germans Trias i Pujol|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia|Spanish Clinical Research Network - SCReN|IrsiCaixa|University of Turin Italy|Instituto de Salud Carlos III|Germans Trias i Pujol Hospital |
October 16 2023 | Phase 2 |
| NCT05198843 | Terminated | Anatomic Stage IV Breast Cancer AJCC v8|Metastatic Triple-Negative Breast Inflammatory Carcinoma |
National Cancer Institute (NCI) |
November 8 2022 | Phase 1|Phase 2 |
| NCT04925648 | Recruiting | Metastatic Prostate Cancer |
St Vincent''s Hospital Sydney |
October 18 2021 | Phase 2 |
질문 1:
What’s the difference between S1021 and S7782? Which one is better for in vivo studies?
답변:
Usually, hydrate will be more stable and dissolve better than free base. But it (S1021) dissolves better in DMSO than hydrate one (S7782).
질문 2:
Can I give it to mice by oral gavage? If so, how to dissolve this compound?
답변:
Our S1021 in 1% DMSO+30% PEG 300+1% Tween 80 at 30 mg/ml is a suspension which you can administrate to mice via oral gavage. If you want a clear solution, it can be dissolved in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5 mg/ml clearly.