Lapatinib Ditosylate
别名: GW-572016 Ditosylate 中文名称：二苯磺酸拉帕替尼
Lapatinib Ditosylate是一种有效的EGFR 和 ErbB2抑制剂，在无细胞试验中IC50分别为10.8和9.2 nM。
Lapatinib Ditosylate Chemical Structure
CAS: 388082-77-7
产品质控
批次：
纯度：
99.99%
99.99
Lapatinib Ditosylate相关产品
| 相关产品 | CP-724714 Sapitinib (AZD8931) Mubritinib (TAK 165) AC480 (BMS-599626) Tyrphostin AG 879 HER2-Inhibitor-1 TAS0728 | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| PC3M | Cytotoxicity assay | 4 days | Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=4.55μM | 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 | |
| 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 | |
| LNCAP | Cytotoxicity assay | 4 days | Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=3.68μM | 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 | |
| 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 | |
| DU145 | Cytotoxicity assay | 4 days | Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=2.99μM | 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 | |
| GXF251L | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=1.48μM | 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 | |
| DIFI | Cytotoxicity assay | 4 days | Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=0.235μM | 22169601 | |
| BT474 | Antiproliferative assay | 3 days | Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50=0.1μM | 22101132 | |
| 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 | 72 hrs | Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50=0.025μM | 21887403 | |
| 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 | 72 hrs | Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50=0.104μM | 19888761 | |
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50=0.029μM | 19888761 | |
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50=0.017μM | 19028425 | |
| 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 | 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells by MTT assay, IC50=42.36μM | 21570843 | ||
| MDA-MB-468 | Antiproliferative assay | Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50=23.46μM | 21570843 | ||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50=4.35μM | 21570843 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50=8.5μM | 21080629 | ||
| HeLa | Cytotoxicity assay | Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50=5.9μM | 21080629 | ||
| A431 | Cytotoxicity assay | Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50=0.97μM | 21080629 | ||
| CAL27 | Cytotoxicity assay | Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50=0.007μM | 21080629 | ||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50=0.003μM | 21080629 | ||
| SKBR3 | Cytotoxicity assay | Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50=0.002μM | 21080629 | ||
| MIAPaCa | Function assay | Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50=0.433μM | 20817523 | ||
| MIAPaCa | Function assay | Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50=0.14μM | 20817523 | ||
| N87 | Function assay | Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50=0.1μM | 20346655 | ||
| A431 | Function assay | Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50=0.052μM | 20346655 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50=6.6μM | 20143778 | ||
| HepG2 | Antiproliferative assay | Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50=6.27μM | 20143778 | ||
| Hep3B2 | Antiproliferative assay | Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50=5.49μM | 20143778 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50=5.4μM | 20143778 | ||
| SKHEP1 | Antiproliferative assay | Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50=5.3μM | 20143778 | ||
| SK-BR-3 | Antiproliferative assay | Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50=0.04μM | 20143778 | ||
| BT474 | Antiproliferative assay | Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50=0.025μM | 18653333 | ||
| HFF cell | Growth inhibition assay | Inhibition of HFF cell growth, IC50=9.9 μM | 16777410 | ||
| N87 cell | Growth inhibition assay | Inhibition of N87 cell growth after 72 hrs, IC50=0.08 μM | 16777410 | ||
| BT474 cell | Growth inhibition assay | Inhibition of BT474 cell growth after 72 hrs, IC50=0.08 μM | 16777410 | ||
| HN5 cell | Growth inhibition assay | Inhibition of HN5 cell growth after 72 hrs, IC50=0.12 μM | 16777410 | ||
| BT474 cell line | Proliferation assay | Antiproliferative activity against human BT474 cell line, IC50=0.025 μM | 16483772 | ||
| HN5 cell line | Proliferation assay | Antiproliferative activity against human HN5 cell line, IC50=0.025 μM | 16483772 | ||
| 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 | ||
| 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 | ||
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50=6.27μM | 29049963 | ||
| 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 | ||
| 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 | ||
| HepG2 | Function assay | Inhibition of EGFR in human HepG2 cells, IC50=0.0271μM | 30096580 | ||
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells, TC50=6.3μM | 30344906 | ||
| 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 | ||
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lapatinib Ditosylate是一种有效的EGFR 和 ErbB2抑制剂，在无细胞试验中IC50分别为10.8和9.2 nM。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Lapatinib 微弱抑制ErbB4活性，IC50为367 nM, 作用于EGFR和 ErbB2 比作用于其他激酶，如c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2,和 VEGFR-2选择性高300多倍。Lapatinib作用于HN5细胞时，显著抑制受体EGFR 和 ErbB2自磷酸化，这种作用存在剂量依赖性，IC50分别为170 nM和80 nM,而作用于BT474细胞时，IC50分别为210 nM 和 60 nM。与OSI-774和Iressa(ZD1839)优先抑制过量表达EGFR细胞生长不同, Lapatinib 抑制过量表达EGFR和ErbB2细胞生长。 作用于过量表达EGFR或 ErbB2的细胞具有高抑制活性，IC50为0.09-0.21 μM,而作用于表达低水平EGFR或ErbB2的细胞，IC50为3-12 μM,比作用于正常纤维细胞选择性高100倍。Lapatinib有效抑制过量表达EGFR的HN5和A-431细胞生长，也抑制过量表达ErbB2的BT474和N87细胞生长，且显著诱导HN5细胞周期停在G1期，也诱导 BT474 细胞凋亡，与抑制AKT磷酸化相关。[1] Lapatinib 作用于含EGFR的L858R和T790M突变的抗Gefitinib的H1975细胞显著抑制Stat3磷酸化，导致细胞生长受抑制，IC50为1-2 μM。[3] | |||
|---|---|---|---|---|
| 激酶实验 | 体外激酶实验 | |||
| 通过测量抑制肽底物磷酸化的情况而获得抑制酶活性的IC50值。通过杆状病毒表达系统纯化EGFR 和 ErbB2的细胞外激酶域。在96孔圆底板上进行EGFR和ErbB2反应，终体积为45 μL。反应混合物含50 mM 4-吗啉丙磺酸(pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi [γ33P] ATP/每次反应, 50 μM 肽 A [生物素-(氨基)-EEEEYFELVAKKK-CONH2], 1 mM 二流苏糖醇，及 1 μL DMSO（含连续稀释的Lapatinib，起始浓度为10 μM）。加入指定纯化的 1型受体胞内域，开始反应。加入的酶量为为1 pmol/每组反应(20 nM)在23oC下反应10分钟，加入45 μL 0.5%溶于水的磷酸，终止反应。终止反应混合物(75 μL) 转移到磷酸纤维过滤板上。板过滤，然后使用200 μL 0.5% 磷酸冲洗3次。每孔加入闪烁剂(50 μL) , 在Packard Topcount上测量每组反应。通过10点剂量反应曲线获得IC50值。 | ||||
| 细胞实验 | 细胞系 | HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, 和 HB4a c5.2 | ||
| 浓度 | 溶于 DMSO,终浓度为~100 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 使用不同浓度Lapatinib处理细胞72小时。使用亚甲基蓝染色测定相对细胞数。使用Spectra酶标仪在620 nm 处测定吸光值。通过碘化丙啶染色和渗透BrdUrd的抗体检测，测量细胞死亡和细胞周期分析。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk pEGFR / EGFR / p-mTOR / mTOR / PARP / c-PARP |
|
25238247 | |
| Growth inhibition assay | Cell viability |
|
24947784 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Lapatinib 按~100 mg/kg剂量口服处理，每天两次，显著抑制BT474和HN5移植瘤生长，这种作用存在剂量依赖性。[1] 与在体外活性一致，Lapatinib按100-150 mg/kg剂量处理携带H1975肿瘤的小鼠，延迟肿瘤生长。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 皮下移植HN5细胞的CD-1雌性裸鼠,皮下移植BT474细胞的 C.B-17 SCID 雌性小鼠 |
| Dosages | ~100 mg/kg | |
| Administration | 口服处理，每天两次 | |
| 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 |
化学信息&溶解度
| 分子量 | 925.46 | 分子式 | C29H26ClFN4O4S.2C7H8O3S |
| CAS号 | 388082-77-7 | SDF | Download Lapatinib Ditosylate SDF |
| 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 185 mg/mL ( (199.9 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
If I need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution?
回答：
S1028 Lapatinib Ditosylate can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution.
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