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Chemical Structure : CEP-37440
CAS No.: 1391712-60-9
Catalog No.: PC-20623Not For Human Use, Lab Use Only.
CEP-37440 (CEP37440) is a potent, selective, and brain penetrant dual FAK/ALK inhibitor with IC50 of 2.0/3.1 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 100 mg | $498 | In stock | |
| 200 mg | $758 | In stock | |
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CEP-37440 (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.
| M.Wt | 580.13 | |
| Formula | C30H38ClN7O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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