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Lapatinib

別名: GSK572016, GW2016 中文名稱：拉帕替尼

Lapatinib 是一種有效的EGFR和ErbB2抑制劑，在無細胞試驗中IC50分別為10.2和9.8 nM。Lapatinib 可誘導(dǎo) ferroptosis 和細胞自噬。

Lapatinib Chemical Structure

Lapatinib Chemical Structure

CAS: 231277-92-2

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
25mg 647.01 現(xiàn)貨
100mg 1392.3 現(xiàn)貨
1g 5487.3 現(xiàn)貨
更大包裝 有超大折扣

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常與Lapatinib一起在實驗中被使用的化合物

Gefitinib

Lapatinib和Gefitinib通過下調(diào)SK-Br-3HER2擴增乳腺癌細胞系中拓撲異構(gòu)酶IIα的表達來誘導(dǎo)耐藥性。

Bhosle J, et al. Mol Cancer Ther. 2013;12(12):2897-2908.

Afatinib

Afatinib通過誘導(dǎo)G1細胞周期停滯和凋亡，在體外比Lapatinib更有效地抑制GLM-1和GLM-1HerR2細胞的生長。

Nakata S, et al. Anticancer Res. 2019 Nov;39(11):5927-5932.

Gemcitabine

Lapatinib和吉西他濱在HER2陽性乳腺癌細胞中表現(xiàn)出協(xié)同抗腫瘤作用。

Matsumoto A, et al.?Mol Med Rep. 2018;18(1):958-964.

Paclitaxel

Lapatinib和Paclitaxel的使用在食管鱗癌中表現(xiàn)出更好的抗腫瘤功效。

Guo XF, et al. Cancer Chemother Pharmacol. 2018;82(3):383-394.

Erlotinib

Lapatinib和Erlotinib通過抑制藥物流出功能逆轉(zhuǎn)MRP7介導(dǎo)的多藥耐藥性。

Kuang YH, et al. Biochem Pharmacol. 2010;79(2):154-161.

Lapatinib相關(guān)產(chǎn)品

相關(guān)信號通路圖

EGFR Signaling Pathways

EGFR信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
A431 Function assay 0.001 to 10 uM 2 hrs Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method 25305330
A431 Function assay 0.001 to 10 uM 2 hrs Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method 25305330
BT474 Function assay 0.001 to 10 uM 2 hrs Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method 25305330
BT474 Function assay 0.001 to 10 uM 2 hrs Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method 25305330
A431 Function assay 0.001 to 10 uM 2 hrs Inhibition of HER1 phosphorylation (unknown origin) expressed in human A431 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method 25305330
BT474 Function assay 0.001 to 10 uM 2 hrs Inhibition of HER2 phosphorylation (unknown origin) expressed in human BT474 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method 25305330
MCF7 Function assay 10 uM 2 hrs Inhibition of HER2 delta16 mutant autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting 24355130
MCF7 Function assay 10 uM 2 hrs Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting 24355130
MCF7 Function assay 10 uM 2 hrs Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2delta16 at 10 uM after 2 hrs by Western blotting 24355130
MCF7 Function assay 10 uM 2 hrs Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2 at 10 uM after 2 hrs by Western blotting 24355130
MCF7 Function assay 10 uM 2 hrs Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting 24355130
MCF7 Function assay 10 uM 2 hrs Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting 24355130
A549 Function assay 50 uM 2 hrs Inhibition of EGFR phosphorylation at Y1068 in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method 28238614
A549 Function assay 50 uM 2 hrs Inhibition of EGFR phosphorylation at Tyr residue in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method 28238614
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 0.011 μM. 25151582
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.017 μM. 19028425
BT474 Antiproliferative assay 72 hrs Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50 = 0.025 μM. 21887403
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.029 μM. 19888761
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay, IC50 = 0.029 μM. 22372864
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0301 μM. 25305330
BT474 Cytotoxicity assay 72 hrs Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay, IC50 = 0.031 μM. 27288180
CAL27 Function assay 16 hrs Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot, IC50 = 0.032 μM. 21080629
NCI-N87 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay, IC50 = 0.036 μM. 22372864
insect cells Function assay 5 mins Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.03755 μM. 30096580
MDA-MB-175 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-175 cells expressing Src, Ret and low HER-2 after 72 hrs by SRB assay, IC50 = 0.0444 μM. 22372864
SK-BR-3 Antiproliferative assay 48 hrs Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.06 μM. 27769671
BT474 Cytotoxicity assay 72 hrs Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0639 μM. 25305330
NCI-N87 Antiproliferative assay 3 days Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining, IC50 = 0.09 μM. 22101132
BT474 Antiproliferative assay 3 days Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50 = 0.1 μM. 22101132
Calu3 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay, IC50 = 0.1 μM. 28092860
BT474 Cytotoxicity assay 48 hrs Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.1 μM. 27769671
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.104 μM. 19888761
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay, IC50 = 0.104 μM. 22372864
HeLa Antiproliferative assay 12 hrs Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.12 μM. 26652482
A431 Antiproliferative assay 48 hrs Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.15 μM. 27769671
MDA-MB-453 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.19 μM. 25305330
BT474 Cytotoxicity assay 72 hrs Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.2 μM. 29089259
B16F10 Antiproliferative assay 12 hrs Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.21 μM. 26652482
Sf21 Function assay 5 mins Inhibition of N-terminal GST-tagged recombinant human EGFR T790M mutant expressed in baculovirus infected Sf21 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.22489 μM. 30096580
Calu3 Cytotoxicity assay 72 hrs Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.23 μM. 25305330
DIFI Cytotoxicity assay 4 days Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.235 μM. 22169601
HepG2 Antiproliferative assay 12 hrs Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.27 μM. 26652482
EOL-1 Cytotoxicity assay 72 hrs Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.41 μM. 29089259
MCF7 Antiproliferative assay 12 hrs Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.47 μM. 26652482
SKBR3 Antiproliferative assay 48 hrs Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.49 μM. 27187856
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.51 μM. 27769671
CAL27 Cytotoxicity assay 4 days Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.53 μM. 22169601
MDA-MB-453 Cytotoxicity assay 72 hrs Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 0.555 μM. 22372864
SKOV3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.59 μM. 25305330
HCC827 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay, IC50 = 0.6 μM. 29421573
A431NS Antiproliferative assay 72 hrs Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay, IC50 = 0.6 μM. 28092860
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.6431 μM. 25305330
BT474 Cytotoxicity assay 72 hrs Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay, GI50 = 0.93 μM. 26475520
MDA-MB-361 Cytotoxicity assay 72 hrs Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 1.029 μM. 22372864
GXF251L Cytotoxicity assay 4 days Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.48 μM. 22169601
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.6 μM. 22595177
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.62 μM. 22182581
LXFA 629L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.87 μM. 22169601
DU145 Cytotoxicity assay 4 days Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.99 μM. 22169601
SKOV3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay, IC50 = 2.99 μM. 22182581
NCI-H1781 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1781 cells expressing HER-2 G776insV_G/C after 72 hrs by SRB assay, IC50 = 3.047 μM. 22372864
OVXF 899L Cytotoxicity assay 4 days Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.35 μM. 22169601
LXFL 529L Cytotoxicity assay 4 days Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.51 μM. 22169601
LNCAP Cytotoxicity assay 4 days Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.68 μM. 22169601
Bel7402 Antiproliferative assay 72 hrs Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. 28092860
LXFA 526L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.21 μM. 22169601
NIH/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50 = 4.3 μM. 22595177
UXF 1138L Cytotoxicity assay 4 days Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.4 μM. 22169601
SK-BR-3 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay, IC50 = 4.4 μM. 28092860
PC3M Cytotoxicity assay 4 days Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.55 μM. 22169601
COLO205 Antiproliferative assay 72 hrs Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay, IC50 = 4.6 μM. 28092860
HT-29 Cytotoxicity assay 4 days Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.62 μM. 22169601
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM. 29421573
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM. 28711703
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 4.8 μM. 28238614
MCF7 Cytotoxicity assay 4 days Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.83 μM. 22169601
MEXF 1341L Cytotoxicity assay 4 days Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.85 μM. 22169601
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay, IC50 = 5.02 μM. 30096580
SKBR3 Antiproliferative assay 72 hrs Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay, IC50 = 5.05 μM. 23927972
SKHEP1 Antiproliferative assay hrs Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 5.3 μM. 20143778
RKO Cytotoxicity assay 4 days Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.35 μM. 22169601
MDA-MB-231 Antiproliferative assay hrs Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50 = 5.4 μM. 20143778
Hep3B2 Antiproliferative assay hrs Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50 = 5.49 μM. 20143778
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 5.7 μM. 29089259
LXFA 289L Cytotoxicity assay 4 days Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.79 μM. 22169601
MAXF 401NL Cytotoxicity assay 4 days Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.8 μM. 22169601
HCT116 Cytotoxicity assay 24 hrs Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay, IC50 = 5.92 μM. 30096580
22Rv1 Cytotoxicity assay 4 days Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.06 μM. 22169601
PAXF 546L Cytotoxicity assay 4 days Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.12 μM. 22169601
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.2 μM. 28092860
NCI-H522 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay, IC50 = 6.4 μM. 28092860
MCF7 Antiproliferative assay hrs Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50 = 6.6 μM. 20143778
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.74 μM. 27187856
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.8 μM. 29684708
PXF 1118L Cytotoxicity assay 4 days Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.86 μM. 22169601
LIXF 575L Cytotoxicity assay 4 days Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.18 μM. 22169601
RXF 1781L Cytotoxicity assay 4 days Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.67 μM. 22169601
MDA231 Cytotoxicity assay 4 days Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.7 μM. 22169601
LXFL 1121L Cytotoxicity assay 4 days Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.73 μM. 22169601
RXF 393NL Cytotoxicity assay 4 days Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.77 μM. 22169601
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 8.1 μM. 29089259
PANC1 Cytotoxicity assay 4 days Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.12 μM. 22169601
CXF 269L Cytotoxicity assay 4 days Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.36 μM. 22169601
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 8.4 μM. 28092860
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 8.468 μM. 25305330
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50 = 9.08 μM. 28711703
NCI-H1975 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 9.08 μM. 28238614
RXF 486L Cytotoxicity assay 4 days Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.1 μM. 22169601
Saos2 Cytotoxicity assay 4 days Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.38 μM. 22169601
PXF 1752L Cytotoxicity assay 4 days Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.46 μM. 22169601
PXF 698L Cytotoxicity assay 4 days Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.49 μM. 22169601
BXF T24 Cytotoxicity assay 4 days Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.65 μM. 22169601
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 10.12 μM. 29684708
MEXF 462NL Cytotoxicity assay 4 days Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.13 μM. 22169601
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. 29684708
TE671 Cytotoxicity assay 4 days Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.95 μM. 22169601
RAW264.7 Antileishmanial assay 96 hrs Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay, EC50 = 11 μM. 28337329
PAXF 1657L Cytotoxicity assay 4 days Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.11 μM. 22169601
MEXF 276L Cytotoxicity assay 4 days Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.37 μM. 22169601
MKN45 Cytotoxicity assay 4 days Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.48 μM. 22169601
BXF 1352L Cytotoxicity assay 4 days Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.53 μM. 22169601
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50 = 11.71 μM. 30096580
BXF 1218L Cytotoxicity assay 4 days Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.77 μM. 22169601
Caco Cytotoxicity assay 24 hrs Cytotoxicity against human Caco cells after 24 hrs by SRB assay, IC50 = 12.11 μM. 30096580
SW480 Antiproliferative assay 72 hrs Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM. 29421573
SW480 Antiproliferative assay 72 hrs Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM. 28711703
SW480 Cytotoxicity assay 72 hrs Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 12.58 μM. 28238614
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50 = 12.68 μM. 29421573
3T3 Antitrypanosomal assay 48 hrs Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay, EC50 = 13 μM. 28337329
HCT116 Cytotoxicity assay 4 days Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.14 μM. 22169601
OVCAR3 Cytotoxicity assay 4 days Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.44 μM. 22169601
H460 Cytotoxicity assay 4 days Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.46 μM. 22169601
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM. 29421573
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM. 28711703
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 14.9 μM. 28238614
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.71 μM. 24355130
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.79 μM. 24355130
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 19.22 μM. 24355130
MDA-MB-468 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay, IC50 = 20 μM. 28092860
HCC827 Cytotoxicity assay 72 hrs Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 22.3 μM. 29089259
ETK-1 Growth Inhibition Assay IC50=10.623 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=10.2565 μM SANGER
TE-15 Growth Inhibition Assay IC50=10.245 μM SANGER
D-247MG Growth Inhibition Assay IC50=9.98291 μM SANGER
HCC2998 Growth Inhibition Assay IC50=9.96307 μM SANGER
KS-1 Growth Inhibition Assay IC50=9.66287 μM SANGER
GCIY Growth Inhibition Assay IC50=9.5742 μM SANGER
D-336MG Growth Inhibition Assay IC50=9.47395 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=9.11675 μM SANGER
TE-8 Growth Inhibition Assay IC50=7.76159 μM SANGER
D-502MG Growth Inhibition Assay IC50=7.48894 μM SANGER
EVSA-T Growth Inhibition Assay IC50=7.42811 μM SANGER
GT3TKB Growth Inhibition Assay IC50=7.22744 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=7.07183 μM SANGER
GI-1 Growth Inhibition Assay IC50=6.51682 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=6.43694 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=6.26561 μM SANGER
NB5 Growth Inhibition Assay IC50=6.21001 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.80046 μM SANGER
COLO-668 Growth Inhibition Assay IC50=5.72667 μM SANGER
SW954 Growth Inhibition Assay IC50=5.39245 μM SANGER
SW962 Growth Inhibition Assay IC50=5.02159 μM SANGER
UACC-812 Growth Inhibition Assay IC50=4.56153 μM SANGER
TK10 Growth Inhibition Assay IC50=4.16522 μM SANGER
TE-5 Growth Inhibition Assay IC50=4.0373 μM SANGER
TE-10 Growth Inhibition Assay IC50=3.55356 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=3.54501 μM SANGER
DJM-1 Growth Inhibition Assay IC50=3.46975 μM SANGER
LS-513 Growth Inhibition Assay IC50=3.40041 μM SANGER
RL95-2 Growth Inhibition Assay IC50=3.1567 μM SANGER
TE-1 Growth Inhibition Assay IC50=2.0483 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=1.99199 μM SANGER
A253 Growth Inhibition Assay IC50=1.97335 μM SANGER
TE-6 Growth Inhibition Assay IC50=1.55201 μM SANGER
LC-1F Growth Inhibition Assay IC50=1.38244 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.36228 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.02544 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.05326 μM SANGER
OCUB-M Growth Inhibition Assay IC50=0.0574 μM SANGER
ECC12 Growth Inhibition Assay IC50=0.09231 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.09396 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.21315 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.24654 μM SANGER
EKVX Growth Inhibition Assay IC50=0.44874 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.49057 μM SANGER
A388 Growth Inhibition Assay IC50=0.72258 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.74453 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=1.15403 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=10.961 μM SANGER
KNS-42 Growth Inhibition Assay IC50=11.7255 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=12.1712 μM SANGER
SR Growth Inhibition Assay IC50=12.2064 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=12.8985 μM SANGER
ES6 Growth Inhibition Assay IC50=13.078 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=13.2577 μM SANGER
D-392MG Growth Inhibition Assay IC50=13.6428 μM SANGER
NB7 Growth Inhibition Assay IC50=14.2374 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=14.5145 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=14.7889 μM SANGER
CA46 Growth Inhibition Assay IC50=15.0586 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=15.1901 μM SANGER
BC-1 Growth Inhibition Assay IC50=15.3314 μM SANGER
LS-123 Growth Inhibition Assay IC50=15.8173 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=16.0924 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=16.7313 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=16.9372 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=17.1529 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=17.4366 μM SANGER
ES7 Growth Inhibition Assay IC50=18.3914 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=18.4386 μM SANGER
SF268 Growth Inhibition Assay IC50=18.7409 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=19.0742 μM SANGER
HCE-T Growth Inhibition Assay IC50=20.2344 μM SANGER
A101D Growth Inhibition Assay IC50=20.8587 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=20.913 μM SANGER
LXF-289 Growth Inhibition Assay IC50=21.038 μM SANGER
NALM-6 Growth Inhibition Assay IC50=21.1967 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=21.4813 μM SANGER
EW-16 Growth Inhibition Assay IC50=22.1402 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=22.2149 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=22.3965 μM SANGER
SKM-1 Growth Inhibition Assay IC50=22.7351 μM SANGER
DMS-153 Growth Inhibition Assay IC50=23.4204 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=23.5452 μM SANGER
LP-1 Growth Inhibition Assay IC50=23.8097 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=24.292 μM SANGER
MPP-89 Growth Inhibition Assay IC50=25.2036 μM SANGER
U-698-M Growth Inhibition Assay IC50=25.2503 μM SANGER
HC-1 Growth Inhibition Assay IC50=25.6418 μM SANGER
HCC2157 Growth Inhibition Assay IC50=25.673 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=26.273 μM SANGER
LS-411N Growth Inhibition Assay IC50=26.3369 μM SANGER
Becker Growth Inhibition Assay IC50=26.5181 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=26.7575 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=27.3867 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=27.4566 μM SANGER
RKO Growth Inhibition Assay IC50=28.1446 μM SANGER
TE-441-T Growth Inhibition Assay IC50=28.789 μM SANGER
EW-24 Growth Inhibition Assay IC50=29.1259 μM SANGER
no-10 Growth Inhibition Assay IC50=29.1631 μM SANGER
D-542MG Growth Inhibition Assay IC50=29.9221 μM SANGER
ST486 Growth Inhibition Assay IC50=30.6451 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=30.8057 μM SANGER
ES8 Growth Inhibition Assay IC50=31.5972 μM SANGER
BL-41 Growth Inhibition Assay IC50=32.1054 μM SANGER
NB6 Growth Inhibition Assay IC50=32.3855 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=32.4967 μM SANGER
MS-1 Growth Inhibition Assay IC50=32.7751 μM SANGER
MFH-ino Growth Inhibition Assay IC50=34.3224 μM SANGER
NOS-1 Growth Inhibition Assay IC50=34.6748 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=35.3667 μM SANGER
EB2 Growth Inhibition Assay IC50=36.6189 μM SANGER
L-540 Growth Inhibition Assay IC50=37.2308 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=38.8846 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=39.9651 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=42.415 μM SANGER
BC-3 Growth Inhibition Assay IC50=45.4896 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=45.5474 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=45.666 μM SANGER
SNB75 Growth Inhibition Assay IC50=46.018 μM SANGER
SKBR3 Cytotoxicity assay Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.002 μM. 21080629
SKOV3 Cytotoxicity assay Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.003 μM. 21080629
CAL27 Cytotoxicity assay Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.007 μM. 21080629
4T1 Cytotoxicity assay Cytotoxicity against mouse triple negative 4T1 cells, IC50 = 0.01037 μM. 24890652
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.02 μM. 24890652
BT474 Antiproliferative assay Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50 = 0.025 μM. 18653333
HEK293 Function assay Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.02706 μM. 28711703
HEK293 Function assay Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.0271 μM. 29421573
HepG2 Function assay Inhibition of EGFR in human HepG2 cells, IC50 = 0.0271 μM. 30096580
MDA-MB-435 Cytotoxicity assay Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.0297 μM. 24890652
SK-BR-3 Antiproliferative assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 0.04 μM. 20143778
A431 Function assay Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.052 μM. 20346655
MCF7 Cytotoxicity assay Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0649 μM. 24890652
MDA-MB-468 Cytotoxicity assay Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.0832 μM. 24890652
N87 Function assay Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 0.1 μM. 20346655
MIAPaCa Function assay Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.14 μM. 20817523
MIAPaCa Function assay Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.433 μM. 20817523
A431 Cytotoxicity assay Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.97 μM. 21080629
SK-BR-3 Antiproliferative assay Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50 = 4.35 μM. 21570843
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 5.9 μM. 21080629
HepG2 Antiproliferative assay Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50 = 6.27 μM. 20143778
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50 = 6.27 μM. 29049963
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells, TC50 = 6.3 μM. 30344906
A549 Cytotoxicity assay Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 8.5 μM. 21080629
MDA-MB-468 Antiproliferative assay Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50 = 23.46 μM. 21570843
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 42.36 μM. 21570843
NCI-N87 Antitumor assay Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor growth inhibition at 20 mg/kg, po QD for 14 days measured after 19 days 22101132
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
NCI-H522 Antitumor assay Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ig administered once daily for 28 days relative to control 28092860
LLC Antitumor assay Antitumor activity against mouse LLC cells implanted in in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 14 days 27187856
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生物活性

產(chǎn)品描述 Lapatinib 是一種有效的EGFR和ErbB2抑制劑，在無細胞試驗中IC50分別為10.2和9.8 nM。Lapatinib 可誘導(dǎo) ferroptosis 和細胞自噬。
特性 Lapatinib 已經(jīng)批準用于治療HER-2陽性轉(zhuǎn)移性乳腺癌。[2]
靶點
ErbB2 [1]
(Cell-free assay)		 EGFR [1]
(Cell-free assay)		 ErbB4 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM
體外研究(In Vitro)
體外研究活性 除了ErbB-4例外, Lapatinib 作用于EGFR 和 ErbB-2比作用于其他測試的激酶，如c-Src, MEK和ERK選擇性高300多倍。Lapatinib處理，抑制EGFR 和ErbB-2受體自磷酸化，這種作用存在劑量依賴性，作用于 BT474 和HN5 細胞時，IC50 分別為 0.17 和? 0.08 μM。Lapatinib作用于EGFR-和ErbB-2-過量表達的腫瘤細胞，抑制EGFR 和ErbB-2自磷酸化，比作用于純化酶的效力低10倍左右。Lapatinib 抑制 EGFR- 和ErbB-2過量表達的細胞生長，而OSI-774和 Iressa（都為EGFR選擇性抑制劑）優(yōu)先抑制 EGFR過量表達的細胞生長。Lapatinib作用于腫瘤細胞比作用于正常成纖維細胞效果高100倍左右。ErbB-2轉(zhuǎn)染的乳腺上皮細胞HB4a c5.2,對 Lapatinib的反應(yīng)敏感度比未轉(zhuǎn)染的親本對照細胞HB4a高40倍左右。使用不含Lapatinib 的培養(yǎng)基培養(yǎng)HN5 細胞群2周左右后，使用30 μM Lapatinib 短暫處理，完全抑制細胞生長。濃度>3.3 μM時抑制50%生長。濃度為0.37 μM時抑制20%生長。另一種EGFR過量表達的細胞A-431, 與HN5反應(yīng)相似。Lapatinib在抑制 EGFR過量表達的細胞生長方面與 OSI-774 相似。[1]
激酶實驗 體外EGFR, ErbB-2,和 ErbB4激酶實驗
從桿狀病毒表達系統(tǒng)中純化EGFR, ErbB-2, 和 ErbB4的細胞內(nèi)激酶域。EGFR, ErbB-2, 和 ErbB-4 反應(yīng)在96孔聚苯乙烯圓底板中進行，終體積為45 μL。反應(yīng)混合物含50 mM 4-嗎啉基丙磺酸(pH 7.5), 2 mM MnCl2,10 μM ATP, 1 μCi [γ-33 P] ATP/每次反應(yīng),50 μM Peptide A [生物素-(氨基酸)-EEEEYFELVAKKK-CONH2],1 mM 二硫蘇糖醇, 及 1 μL 含連續(xù)稀釋Lapatinib（初濃度為10 μM）的 DMSO。加入指定純化的1型受體細胞內(nèi)域開始反應(yīng)。加入的酶量為1 pmol/每次反應(yīng) (20 nM)。在23oC反應(yīng)10分鐘，加入溶于水的 45 μL 0.5% 磷酸后，終止反應(yīng)。最終反應(yīng)混合物(75 μL) 轉(zhuǎn)移到磷酸纖維素過濾板上。過濾實驗板，使用200 μL 0.5% 磷酸沖洗三次。每孔中加入閃爍混合物(50 μL),使用Packard Topcount計數(shù)而量化實驗結(jié)果。
細胞實驗 細胞系 HFF , BT474, MCF-7, N87, CaLu-3, HN5, A-431, T47D, HB4a, 和 HB4a c5.2
濃度 0 到 100 nM
孵育時間 3 天
方法 按以下密度接種細胞：HFF, 1.5×104 個細胞/cm2; BT474, MCF-7, N87, 和 CaLu-3, 3×104 個細胞/cm2; 及HN5, A-431, T47D, HB4a, 和 HB4a c5.2, 1×104 個細胞/cm2，使在實驗期間細胞處于對數(shù)生長期。24 小時后,使用濃度范圍為0 到 100 nM的Lapatinib處理細胞。在含5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的低糖DMEM培養(yǎng)基中處理HFF, BT474,HN5, 和 N87 細胞。在50% 高糖DMEM,和50%含5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的低糖DMEM中處理MCF-7細胞。在 50% RPMI,50%含 5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO 的低糖DMEM中處理T47D, A-431, 和CaLu-3 細胞。在50% DMEM, 50% 含5% FBS, 2.5 μg/mL hydrocortisone, 2.5 μg/mL 胰島素, 25 μg/mL hygromycin B, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的RPMI 1640中處理HB4a 和 HB4a c5.2細胞。3天后, 使用亞甲基藍染色測評相對細胞數(shù)。移除培養(yǎng)基，每孔加入溶解在 50% 乙醇和50% 水中的100 μL 0.5% w/v亞甲基藍。浸泡在去離子水中洗滌實驗板，然后在空氣中烘干。每孔加入溶解在PBS的1% w/v n-lauroylsarcosine(100 μL), 然后實驗板在室溫下溫育30分鐘。使用Spectra酶標儀在620 nm處測定吸光值。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1 29799521
Immunofluorescence LC3 Vimentin / E-cadherin 26637440
Growth inhibition assay Cell viability (OE19) Cell viability (A431 cells) 25350844
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Lapatinib有效抑制BT474 和HN5 人類移植瘤生長。使用30和 100 mg/kg Lapatinib 口服給藥攜帶腫瘤的小鼠，每天兩次，抑制腫瘤生長，這種作用存在劑量依賴性。按100 mg/kg 劑量處理完全抑制腫瘤生長。按這種劑量處理，在處理21天期間，有<10%腫瘤損失。[1]
動物實驗 Animal Models 雌性CD-1裸鼠和雌性C.B-17 SCID 小鼠
Dosages 100 mg/kg
Administration 口服，每天兩次
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

化學(xué)信息&溶解度

分子量 581.06 分子式

C29H26ClFN4O4S
CAS號 231277-92-2 SDF Download Lapatinib SDF
Smiles CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (172.09 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
If I want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

回答：
For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

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