Home Protein Tyrosine Kinase EGFR 억제제 Lapatinib (GW572016)

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Lapatinib (GW572016) EGFR/HER2 억제제

제품 번호S2111

Lapatinib은 세포 유리 분석에서 IC50이 각각 10.8 및 9.2 nM인 강력한 EGFR 및 ErbB2 억제제입니다. Lapatinib은 Ferroptosis 및 autophagic cell death를 유도합니다.
Lapatinib (GW572016) EGFR 억제제 Chemical Structure

화학 구조

분자량: 581.06

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품질 관리

배치: 순도: 99.95%
99.95

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
LB2241-RCC Growth Inhibition Assay IC50=1.15403 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.74453 μM SANGER
A388 Growth Inhibition Assay IC50=0.72258 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.49057 μM SANGER
EKVX Growth Inhibition Assay IC50=0.44874 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.24654 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.21315 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.09396 μM SANGER
ECC12 Growth Inhibition Assay IC50=0.09231 μM SANGER
OCUB-M Growth Inhibition Assay IC50=0.0574 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.05326 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.02544 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.36228 μM SANGER
LC-1F Growth Inhibition Assay IC50=1.38244 μM SANGER
TE-6 Growth Inhibition Assay IC50=1.55201 μM SANGER
A253 Growth Inhibition Assay IC50=1.97335 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=1.99199 μM SANGER
TE-1 Growth Inhibition Assay IC50=2.0483 μM SANGER
RL95-2 Growth Inhibition Assay IC50=3.1567 μM SANGER
LS-513 Growth Inhibition Assay IC50=3.40041 μM SANGER
DJM-1 Growth Inhibition Assay IC50=3.46975 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=3.54501 μM SANGER
TE-10 Growth Inhibition Assay IC50=3.55356 μM SANGER
TE-5 Growth Inhibition Assay IC50=4.0373 μM SANGER
TK10 Growth Inhibition Assay IC50=4.16522 μM SANGER
UACC-812 Growth Inhibition Assay IC50=4.56153 μM SANGER
SW962 Growth Inhibition Assay IC50=5.02159 μM SANGER
SW954 Growth Inhibition Assay IC50=5.39245 μM SANGER
COLO-668 Growth Inhibition Assay IC50=5.72667 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.80046 μM SANGER
NB5 Growth Inhibition Assay IC50=6.21001 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=6.26561 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=6.43694 μM SANGER
GI-1 Growth Inhibition Assay IC50=6.51682 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=7.07183 μM SANGER
GT3TKB Growth Inhibition Assay IC50=7.22744 μM SANGER
EVSA-T Growth Inhibition Assay IC50=7.42811 μM SANGER
D-502MG Growth Inhibition Assay IC50=7.48894 μM SANGER
TE-8 Growth Inhibition Assay IC50=7.76159 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=9.11675 μM SANGER
D-336MG Growth Inhibition Assay IC50=9.47395 μM SANGER
GCIY Growth Inhibition Assay IC50=9.5742 μM SANGER
KS-1 Growth Inhibition Assay IC50=9.66287 μM SANGER
HCC2998 Growth Inhibition Assay IC50=9.96307 μM SANGER
D-247MG Growth Inhibition Assay IC50=9.98291 μM SANGER
TE-15 Growth Inhibition Assay IC50=10.245 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=10.2565 μM SANGER
ETK-1 Growth Inhibition Assay IC50=10.623 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=10.961 μM SANGER
KNS-42 Growth Inhibition Assay IC50=11.7255 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=12.1712 μM SANGER
SR Growth Inhibition Assay IC50=12.2064 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=12.8985 μM SANGER
ES6 Growth Inhibition Assay IC50=13.078 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=13.2577 μM SANGER
D-392MG Growth Inhibition Assay IC50=13.6428 μM SANGER
NB7 Growth Inhibition Assay IC50=14.2374 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=14.5145 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=14.7889 μM SANGER
CA46 Growth Inhibition Assay IC50=15.0586 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=15.1901 μM SANGER
BC-1 Growth Inhibition Assay IC50=15.3314 μM SANGER
LS-123 Growth Inhibition Assay IC50=15.8173 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=16.0924 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=16.7313 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=16.9372 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=17.1529 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=17.4366 μM SANGER
ES7 Growth Inhibition Assay IC50=18.3914 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=18.4386 μM SANGER
SF268 Growth Inhibition Assay IC50=18.7409 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=19.0742 μM SANGER
HCE-T Growth Inhibition Assay IC50=20.2344 μM SANGER
A101D Growth Inhibition Assay IC50=20.8587 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=20.913 μM SANGER
LXF-289 Growth Inhibition Assay IC50=21.038 μM SANGER
NALM-6 Growth Inhibition Assay IC50=21.1967 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=21.4813 μM SANGER
EW-16 Growth Inhibition Assay IC50=22.1402 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=22.2149 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=22.3965 μM SANGER
SKM-1 Growth Inhibition Assay IC50=22.7351 μM SANGER
DMS-153 Growth Inhibition Assay IC50=23.4204 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=23.5452 μM SANGER
LP-1 Growth Inhibition Assay IC50=23.8097 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=24.292 μM SANGER
MPP-89 Growth Inhibition Assay IC50=25.2036 μM SANGER
U-698-M Growth Inhibition Assay IC50=25.2503 μM SANGER
HC-1 Growth Inhibition Assay IC50=25.6418 μM SANGER
HCC2157 Growth Inhibition Assay IC50=25.673 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=26.273 μM SANGER
LS-411N Growth Inhibition Assay IC50=26.3369 μM SANGER
Becker Growth Inhibition Assay IC50=26.5181 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=26.7575 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=27.3867 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=27.4566 μM SANGER
RKO Growth Inhibition Assay IC50=28.1446 μM SANGER
TE-441-T Growth Inhibition Assay IC50=28.789 μM SANGER
EW-24 Growth Inhibition Assay IC50=29.1259 μM SANGER
no-10 Growth Inhibition Assay IC50=29.1631 μM SANGER
D-542MG Growth Inhibition Assay IC50=29.9221 μM SANGER
ST486 Growth Inhibition Assay IC50=30.6451 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=30.8057 μM SANGER
ES8 Growth Inhibition Assay IC50=31.5972 μM SANGER
BL-41 Growth Inhibition Assay IC50=32.1054 μM SANGER
NB6 Growth Inhibition Assay IC50=32.3855 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=32.4967 μM SANGER
MS-1 Growth Inhibition Assay IC50=32.7751 μM SANGER
MFH-ino Growth Inhibition Assay IC50=34.3224 μM SANGER
NOS-1 Growth Inhibition Assay IC50=34.6748 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=35.3667 μM SANGER
EB2 Growth Inhibition Assay IC50=36.6189 μM SANGER
L-540 Growth Inhibition Assay IC50=37.2308 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=38.8846 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=39.9651 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=42.415 μM SANGER
BC-3 Growth Inhibition Assay IC50=45.4896 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=45.5474 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=45.666 μM SANGER
SNB75 Growth Inhibition Assay IC50=46.018 μM SANGER
SKBR3 Cytotoxicity assay Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.002 μM. 21080629
SKOV3 Cytotoxicity assay Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.003 μM. 21080629
CAL27 Cytotoxicity assay Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.007 μM. 21080629
4T1 Cytotoxicity assay Cytotoxicity against mouse triple negative 4T1 cells, IC50 = 0.01037 μM. 24890652
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 0.011 μM. 25151582
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.017 μM. 19028425
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.02 μM. 24890652
BT474 Antiproliferative assay Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50 = 0.025 μM. 18653333
BT474 Antiproliferative assay 72 hrs Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50 = 0.025 μM. 21887403
HEK293 Function assay Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.02706 μM. 28711703
HEK293 Function assay Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.0271 μM. 29421573
HepG2 Function assay Inhibition of EGFR in human HepG2 cells, IC50 = 0.0271 μM. 30096580
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.029 μM. 19888761
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay, IC50 = 0.029 μM. 22372864
MDA-MB-435 Cytotoxicity assay Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.0297 μM. 24890652
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0301 μM. 25305330
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 = 0.031 μM. 27288180
CAL27 Function assay 16 hrs Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot, IC50 = 0.032 μM. 21080629
NCI-N87 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay, IC50 = 0.036 μM. 22372864
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 = 0.03755 μM. 30096580
SK-BR-3 Antiproliferative assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 0.04 μM. 20143778
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 = 0.0444 μM. 22372864
A431 Function assay Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.052 μM. 20346655
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 = 0.06 μM. 27769671
BT474 Cytotoxicity assay 72 hrs Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0639 μM. 25305330
MCF7 Cytotoxicity assay Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0649 μM. 24890652
MDA-MB-468 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.0832 μM. 24890652
NCI-N87 Antiproliferative assay 3 days Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining, IC50 = 0.09 μM. 22101132
N87 Function assay Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 0.1 μM. 20346655
BT474 Antiproliferative assay 3 days Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50 = 0.1 μM. 22101132
Calu3 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay, IC50 = 0.1 μM. 28092860
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 = 0.1 μM. 27769671
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.104 μM. 19888761
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay, IC50 = 0.104 μM. 22372864
HeLa Antiproliferative assay 12 hrs Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.12 μM. 26652482
MIAPaCa Function assay Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.14 μM. 20817523
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 = 0.15 μM. 27769671
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 = 0.19 μM. 25305330
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 = 0.2 μM. 29089259
B16F10 Antiproliferative assay 12 hrs Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.21 μM. 26652482
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 = 0.22489 μM. 30096580
Calu3 Cytotoxicity assay 72 hrs Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.23 μM. 25305330
DIFI Cytotoxicity assay 4 days Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.235 μM. 22169601
HepG2 Antiproliferative assay 12 hrs Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.27 μM. 26652482
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 = 0.41 μM. 29089259
MIAPaCa Function assay Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.433 μM. 20817523
MCF7 Antiproliferative assay 12 hrs Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.47 μM. 26652482
SKBR3 Antiproliferative assay 48 hrs Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.49 μM. 27187856
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 = 0.51 μM. 27769671
CAL27 Cytotoxicity assay 4 days Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.53 μM. 22169601
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 = 0.555 μM. 22372864
SKOV3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.59 μM. 25305330
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay, IC50 = 0.6 μM. 29421573
A431NS Antiproliferative assay 72 hrs Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay, IC50 = 0.6 μM. 28092860
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.6431 μM. 25305330
BT474 Cytotoxicity assay 72 hrs Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay, GI50 = 0.93 μM. 26475520
A431 Cytotoxicity assay Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.97 μM. 21080629
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 = 1.029 μM. 22372864
GXF251L Cytotoxicity assay 4 days Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.48 μM. 22169601
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.6 μM. 22595177
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.62 μM. 22182581
LXFA 629L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.87 μM. 22169601
DU145 Cytotoxicity assay 4 days Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.99 μM. 22169601
SKOV3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay, IC50 = 2.99 μM. 22182581
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 = 3.047 μM. 22372864
OVXF 899L Cytotoxicity assay 4 days Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.35 μM. 22169601
LXFL 529L Cytotoxicity assay 4 days Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.51 μM. 22169601
LNCAP Cytotoxicity assay 4 days Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.68 μM. 22169601
Bel7402 Antiproliferative assay 72 hrs Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. 28092860
LXFA 526L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.21 μM. 22169601
NIH/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50 = 4.3 μM. 22595177
SK-BR-3 Antiproliferative assay Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50 = 4.35 μM. 21570843
UXF 1138L Cytotoxicity assay 4 days Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.4 μM. 22169601
SK-BR-3 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay, IC50 = 4.4 μM. 28092860
PC3M Cytotoxicity assay 4 days Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.55 μM. 22169601
COLO205 Antiproliferative assay 72 hrs Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay, IC50 = 4.6 μM. 28092860
HT-29 Cytotoxicity assay 4 days Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.62 μM. 22169601
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM. 29421573
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM. 28711703
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 4.8 μM. 28238614
MCF7 Cytotoxicity assay 4 days Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.83 μM. 22169601
MEXF 1341L Cytotoxicity assay 4 days Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.85 μM. 22169601
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay, IC50 = 5.02 μM. 30096580
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 = 5.05 μM. 23927972
SKHEP1 Antiproliferative assay hrs Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 5.3 μM. 20143778
RKO Cytotoxicity assay 4 days Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.35 μM. 22169601
MDA-MB-231 Antiproliferative assay hrs Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50 = 5.4 μM. 20143778
Hep3B2 Antiproliferative assay hrs Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50 = 5.49 μM. 20143778
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 = 5.7 μM. 29089259
LXFA 289L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.79 μM. 22169601
MAXF 401NL Cytotoxicity assay 4 days Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.8 μM. 22169601
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 5.9 μM. 21080629
HCT116 Cytotoxicity assay 24 hrs Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay, IC50 = 5.92 μM. 30096580
22Rv1 Cytotoxicity assay 4 days Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.06 μM. 22169601
PAXF 546L Cytotoxicity assay 4 days Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.12 μM. 22169601
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.2 μM. 28092860
HepG2 Antiproliferative assay Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50 = 6.27 μM. 20143778
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50 = 6.27 μM. 29049963
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells, TC50 = 6.3 μM. 30344906
NCI-H522 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay, IC50 = 6.4 μM. 28092860
MCF7 Antiproliferative assay hrs Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50 = 6.6 μM. 20143778
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.74 μM. 27187856
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.8 μM. 29684708
PXF 1118L Cytotoxicity assay 4 days Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.86 μM. 22169601
LIXF 575L Cytotoxicity assay 4 days Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.18 μM. 22169601
RXF 1781L Cytotoxicity assay 4 days Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.67 μM. 22169601
MDA231 Cytotoxicity assay 4 days Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.7 μM. 22169601
LXFL 1121L Cytotoxicity assay 4 days Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.73 μM. 22169601
RXF 393NL Cytotoxicity assay 4 days Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.77 μM. 22169601
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 = 8.1 μM. 29089259
PANC1 Cytotoxicity assay 4 days Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.12 μM. 22169601
CXF 269L Cytotoxicity assay 4 days Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.36 μM. 22169601
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 8.4 μM. 28092860
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 8.468 μM. 25305330
A549 Cytotoxicity assay Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 8.5 μM. 21080629
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 = 9.08 μM. 28711703
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 = 9.08 μM. 28238614
RXF 486L Cytotoxicity assay 4 days Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.1 μM. 22169601
Saos2 Cytotoxicity assay 4 days Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.38 μM. 22169601
PXF 1752L Cytotoxicity assay 4 days Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.46 μM. 22169601
PXF 698L Cytotoxicity assay 4 days Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.49 μM. 22169601
BXF T24 Cytotoxicity assay 4 days Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.65 μM. 22169601
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 10.12 μM. 29684708
MEXF 462NL Cytotoxicity assay 4 days Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.13 μM. 22169601
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. 29684708
TE671 Cytotoxicity assay 4 days Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.95 μM. 22169601
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 = 11 μM. 28337329
PAXF 1657L Cytotoxicity assay 4 days Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.11 μM. 22169601
MEXF 276L Cytotoxicity assay 4 days Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.37 μM. 22169601
MKN45 Cytotoxicity assay 4 days Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.48 μM. 22169601
BXF 1352L Cytotoxicity assay 4 days Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.53 μM. 22169601
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50 = 11.71 μM. 30096580
BXF 1218L Cytotoxicity assay 4 days Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.77 μM. 22169601
Caco Cytotoxicity assay 24 hrs Cytotoxicity against human Caco cells after 24 hrs by SRB assay, IC50 = 12.11 μM. 30096580
SW480 Antiproliferative assay 72 hrs Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM. 29421573
SW480 Antiproliferative assay 72 hrs Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM. 28711703
SW480 Cytotoxicity assay 72 hrs Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 12.58 μM. 28238614
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 = 12.68 μM. 29421573
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 = 13 μM. 28337329
HCT116 Cytotoxicity assay 4 days Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.14 μM. 22169601
OVCAR3 Cytotoxicity assay 4 days Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.44 μM. 22169601
H460 Cytotoxicity assay 4 days Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.46 μM. 22169601
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 = 14.9 μM. 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 = 14.9 μM. 28711703
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 14.9 μM. 28238614
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 = 15.71 μM. 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 = 15.79 μM. 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 = 19.22 μM. 24355130
MDA-MB-468 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay, IC50 = 20 μM. 28092860
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 = 22.3 μM. 29089259
MDA-MB-468 Antiproliferative assay Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50 = 23.46 μM. 21570843
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 42.36 μM. 21570843
NCI-N87 Antitumor assay 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
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
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
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
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
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 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
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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
NCI-H522 Antitumor assay 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
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 expressing pcDNA3 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 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 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting 24355130
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
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
LLC Antitumor assay 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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 581.06 화학식

C29H26ClFN4O4S

 보관 (수령일로부터)
CAS 번호 231277-92-2 SDF 다운로드 원액 보관

동의어 GSK572016, GW2016 Smiles 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

In vitro
배치:

DMSO : 100 mg/mL (172.09 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

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

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)
Lapatinib은 367 nM의 IC50으로 ErbB4 활성을 약하게 억제하며, c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2 및 VEGFR2와 같은 다른 키나아제에 비해 EGFR 및 ErbB2에 대해 300배 이상의 선택성을 보입니다. 이 화합물은 HN5 세포에서 EGFR 및 ErbB2의 수용체 자가인산화를 용량 의존적으로 유의하게 억제하며 각각 170 nM 및 80 nM의 IC50을 가집니다. 또한 BT474 세포에서는 각각 210 nM 및 60 nM의 IC50을 가집니다. EGFR 과발현 세포의 성장을 preferentially 억제하는 OSI-774 및 Iressa (ZD1839)와 달리, EGFR 및 ErbB2 과발현 세포의 성장을 모두 억제합니다. 이 화학물질은 EGFR 또는 ErbB2 과발현 세포에 대해 0.09-0.21 μM의 IC50으로 더 높은 억제 활성을 보이며, EGFR 또는 ErbB2 발현 수준이 낮은 세포 (IC50 3-12 μM)에 비해 정상 섬유아세포에 대해 ~100배의 선택성을 나타냅니다. 이는 EGFR 과발현 HN5 및 A-431 세포, 그리고 ErbB2 과발현 BT474 및 N87 세포의 성장을 강력하게 억제하며, HN5 세포의 G1기 정지와 BT474 세포의 apoptosis를 유의하게 유도하는데, 이는 AKT 인산화 억제와 관련이 있습니다.
키나아제 분석
시험관 내 키나아제 분석
효소 활성 억제에 대한 IC50 값은 펩타이드 기질의 인산화 억제를 측정하여 생성됩니다. EGFR 및 ErbB2의 세포내 키나아제 도메인은 바큘로바이러스 발현 시스템에서 정제됩니다. EGFR 및 ErbB2 반응은 96웰 폴리스티렌 둥근 바닥 플레이트에서 최종 부피 45 μL로 수행됩니다. 반응 혼합물은 50 mM 4-모르폴린프로판술폰산 (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi [γ33P] ATP/반응, 50 μM 펩타이드 A [바이오틴-(아미노 헥사노산)-EEEEYFELVAKKK-CONH2], 1 mM 디티오트레이톨 및 10 μM에서 시작하는 이 화합물의 연속 희석액을 포함하는 1 μL DMSO를 함유합니다. 반응은 지정된 정제된 유형-1 수용체 세포내 도메인을 추가하여 시작됩니다. 추가된 효소의 양은 반응당 1 pmol (20 nM)입니다. 반응은 23°C에서 10분 후 45 μL의 0.5% 인산을 물에 첨가하여 종료됩니다. 종료된 반응 혼합물 (75 μL)은 포스포셀룰로스 필터 플레이트로 옮겨집니다. 플레이트는 필터링되고 200 μL의 0.5% 인산으로 세 번 세척됩니다. 섬광 칵테일 (50 μL)이 각 웰에 첨가되고, 분석은 Packard Topcount에서 계수하여 정량화됩니다. IC50 값은 10점 용량-반응 곡선에서 생성됩니다.
생체 내(In vivo)
Lapatinib (~100 mg/kg)을 1일 2회 경구 투여하면 BT474 및 HN5 이종 이식편의 성장을 용량 의존적으로 유의하게 억제합니다.
참조

적용 분야

방법 바이오마커 이미지 PMID
Western blot ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1
S2111-WB1
29799521
Immunofluorescence LC3 Vimentin / E-cadherin
S2111-IF1
26637440
Growth inhibition assay Cell viability (OE19) Cell viability (A431 cells)
S2111-viability1
25350844

임상시험 정보

(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

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자주 묻는 질문

질문 1:
If I want to use this compound via injection in tumor-bearing mice, how could I prepare the solution?

답변:
For I.P. administration, the compound solution should be clear solution. It can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.