Tepotinib (EMD1214063, MSC2156119)

Chemical Structure : Tepotinib

CAS No.: 1100598-32-0

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货号: PC-20461Not For Human Use, Lab Use Only.

Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated variants.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg	￥5280	In stock
250 mg		Get quote

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Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of c-MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated variants.
EMD1214063 displays higher IC50 values for V1206L, L1213V, and Y1248H variants (224.0, 270.1, and >1,000 nM, respectively), reduces the receptor Tyr1234/1235 autophosphorylation in NIH3T3 cell lines.
EMD1214063 inhibits the activation state of the MET downstream signaling molecules AKT, ERK, and PLCγ with IC50 of <75 nM in NIH3T3 mouse fibroblast cells stably expressing distinct MET-activating point mutations.
EMD1214063 selectively attenuates MET-dependent cell-cycle progression of cell lines expressing drug-sensitive forms of the MET receptor, shows high sensitivity agianst variants V1238I, M1268T, and H1112L (30 nM).
EMD1214063 (50 mg/kg/d) represses tumor growth in MET-driven xenograft drug-sensitive tumors bearing the H1112L MET mutation but not the drug-resistant MET mutants L1213V.

物理化学性质&存储条件

分子量	492.58
分子式	C29H28N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(1-(3-(5-((1-methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile

参考文献

1. Medová M, et al. Mol Cancer Ther. 2013 Nov;12(11):2415-24.

2. Bill KL, et al. Lab Invest. 2015 Aug;95(8):951-61.

3. Bladt F, et al. Clin Cancer Res. 2013;19:2941–51.