CEP-37440 (ESK440) | FAK/ALK inhibitor | Probechem Biochemicals

Chemical Structure : CEP-37440

CAS No.: 1391712-60-9

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CEP-37440 (ESK440, CEP37440)

货号: PC-20623Not For Human Use, Lab Use Only.

CEP-37440 (ESK440, CEP37440) is a potent, selective, and brain penetrant dual FAK/ALK inhibitor with IC50 of 2.0/3.1 nM, respectively.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg		Get quote

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生物&药学活性

CEP-37440 (ESK440, CEP37440) is a potent, selective, and brain penetrant dual FAK/ALK inhibitor with IC50 of 2.0/3.1 nM, respectively.
CEP-37440 exhibits a Kd value of 3.6 nM for ALK (WT), displays similar potencies for the ALK mutants ALK (1151Tins, Kd 2.6 nM), ALK (C1156Y, Kd=1.6 nM), ALK (F1174L, Kd=1.1 nM, as well as the gatekeeper mutation ALK (L1196M, Kd=3.3 nM).
CEP-37440 exhibits selectivity against the full DiscoveRx kinase panel (442 kinases) at 1 uM.
CEP-37440 at low concentration decreases the proliferation of the IBC cell lines FC-IBC02, SUM190, and KPL4, while not affecting the proliferation of normal breast epithelial cells.
CEP-37440 decreases the cell proliferation of FC-IBC02, SUM190, and KPL4 by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397).
CEP-37440 affects the expression of genes related to apoptosis, affects the expression of genes related to apoptosis, interferon signaling, and cytokines, exhibits SUM190, FC-IBC02, and SUM149 breast tumor xenografts.

物理化学性质&存储条件

分子量	580.13
分子式	C30H38ClN7O3
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	2-[[5-Chloro-2-[[(6S)-6,7,8,9-tetrahydro-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-N-methylbenzamide

参考文献

1. Ott GR, et al. J Med Chem. 2016 Aug 25;59(16):7478-96.

2. Salem I, et al. Breast Cancer Res. 2016 Mar 24;18(1):37.

CEP-37440 (ESK440, CEP37440)

生物&药学活性

物理化学性质&存储条件

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CEP-37440 (ESK440, CEP37440)

生物&药学活性

物理化学性质&存储条件

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