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Lapatinib Ditosylate HER2 Inibitore

Name: Lapatinib Ditosylate
Brand: Selleck Chemicals
SKU: S1028
Rating: 5 (143 reviews)

N. Cat.: S1028

Lapatinib Ditosilato è un potente inibitore di EGFR ed ErbB2 con IC50 di 10,8 e 9,2 nM in saggi acellulari, rispettivamente.

Lapatinib Ditosylate HER2 Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 925.46

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.98%

99.98

Target correlati	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 c-Kit
Altro HER2 Inibitori	Sevabertinib (BAY 2927088) CP-724714 Sapitinib (AZD8931) Mubritinib (TAK 165) AC480 (BMS-599626) Tyrphostin AG 879 HER2-Inhibitor-1 TAS0728 Zongertinib (BI 1810631)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	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
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	925.46	Formula	C₂₉H₂₆ClFN₄O₄S.2C₇H₈O₃S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	388082-77-7	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 186 mg/mL (200.98 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	1.250mg/ml (1.35mM)	Taking the 1 mL working solution as an example, add 20 μL 62.5 mg/ml clear DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 530 μL ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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 Ditosilato inibisce debolmente l'attività di ErbB4 con IC50 di 367 nM e mostra una selettività >300 volte superiore per EGFR ed ErbB2 rispetto ad altre chinasi come c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2 e VEGFR2. Questo composto inibisce significativamente l'autofosforilazione del recettore di EGFR ed ErbB2 in modo dose-dipendente con IC50 di 170 nM e 80 nM, rispettivamente nelle cellule HN5; così come 210 nM e 60 nM, rispettivamente nelle cellule BT474. A differenza di OSI-774 e Iressa (ZD1839) che inibiscono preferenzialmente la crescita delle cellule che sovraesprimono EGFR, inibisce la crescita di cellule che sovraesprimono sia EGFR che ErbB2. Mostra una maggiore attività inibitoria contro le cellule che sovraesprimono EGFR o ErbB2 con IC50 di 0,09-0,21 μM, rispetto alle cellule che esprimono bassi livelli di EGFR o ErbB2 con IC50 di 3-12 μM, ed esibisce una selettività di circa 100 volte rispetto alle normali cellule fibroblastiche. Questa sostanza chimica inibisce potentemente la crescita delle cellule HN5 e A-431 che sovraesprimono EGFR, così come delle cellule BT474 e N87 che sovraesprimono ErbB2, e induce significativamente l'arresto in fase G1 delle cellule HN5 e l'apoptosi delle cellule BT474, che sono associate all'inibizione della fosforilazione di AKT.
Saggio chinasico	Saggi chinasici in vitro
Saggio chinasico	I valori di IC50 per l'inibizione dell'attività enzimatica sono generati misurando l'inibizione della fosforilazione di un substrato peptidico. I domini chinasici intracellulari di EGFR ed ErbB2 sono purificati da un sistema di espressione con baculovirus. Le reazioni di EGFR ed ErbB2 vengono eseguite in piastre di polistirene a 96 pozzetti con fondo arrotondato in un volume finale di 45 μL. Le miscele di reazione contengono 50 mM di acido 4-morfolinopropansolfonico (pH 7,5), 2 mM di MnCl₂, 10 μM di ATP, 1 μCi di [γ³³P] ATP/reazione, 50 μM di Peptide A [Biotina-(acido amino esanoico)-EEEEYFELVAKKK-CONH2], 1 mM di ditiotreitolo e 1 μL di DMSO contenente diluizioni seriali di questo composto a partire da 10 μM. La reazione viene avviata aggiungendo il dominio intracellulare del recettore di tipo 1 purificato indicato. La quantità di enzima aggiunta è di 1 pmol/reazione (20 nM). Le reazioni vengono terminate dopo 10 minuti a 23°C aggiungendo 45 μL di acido fosforico allo 0,5% in acqua. La miscela di reazione terminata (75 μL) viene trasferita su piastre filtranti di fosfocellulosa. Le piastre vengono filtrate e lavate tre volte con 200 μL di acido fosforico allo 0,5%. Un cocktail scintillante (50 μL) viene aggiunto a ciascun pozzetto e il saggio viene quantificato tramite conteggio in un Packard Topcount. I valori di IC50 sono generati da curve dose-risposta a 10 punti.
In vivo	La somministrazione orale di Lapatinib Ditosilato (~100 mg/kg) due volte al giorno inibisce significativamente la crescita di xenotrapianti BT474 e HN5 in modo dose-dipendente.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/12467226/

Applicazioni (Applications)

Metodi	Biomarcatori	Immagini	PMID
Western blot	pEGFR / EGFR / p-mTOR / mTOR / PARP / c-PARP p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk		28938602
Growth inhibition assay	Cell viability		24947784

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Domande Frequenti (Frequently Asked Questions)

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

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

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