Home Protein Tyrosine Kinase HER2 inhibitor Lapatinib Ditosylate

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Lapatinib Ditosylate HER2 inhibitor

Cat.No.S1028

Lapatinib Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Lapatinib Ditosylate HER2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 925.46

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Quality Control

Batch: Purity: 99.98%
99.98

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 186 mg/mL (200.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 925.46 Formula

C29H26ClFN4O4S.2C7H8O3S

 Storage (From the date of receipt)
CAS No. 388082-77-7 Download SDF Storage of Stock Solutions

Synonyms 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

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
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.
Kinase Assay
In vitro kinase assays
The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of this compound beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.
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.
References

Applications

Methods Biomarkers Images PMID
Western blot p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk pEGFR / EGFR / p-mTOR / mTOR / PARP / c-PARP
S1028-WB1
25238247
Growth inhibition assay Cell viability
S1028-viability1
24947784

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

Question 1:
If I need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution?

Answer:
It can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution.

Signaling Pathway Map