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CEP-37440

Names

[ CAS No. ]:
1391712-60-9

[ Name ]:
CEP-37440

[Synonym ]:
2-(5-chloro-2-{(S)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1-methoxy-6,7,8,9-tetrahydro-5H-benzocyclohepten-2-ylamino}pyrimidin-4-ylamino)-N-methylbenzamide
2-[[5-chloro-2-[[(6S)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1-methoxy-6,7,8,9-tetrahydro-5Hbenzo[7]annulen-2-yl]amino]pyrimidin-4-yl]amino]-N-methyl-benzamide
2-{[5-Chloro-2-({(6R)-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl}amino)-4-pyrimidinyl]amino}-N-methylbenzamide
Benzamide, 2-[[5-chloro-2-[[(6R)-6,7,8,9-tetrahydro-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-N-methyl-
Benzamide, 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-methyl-
2-[[5-chloro-2-[[(6S)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]-amino]pyrimidin-4-yl]amino]-N-methylbenzamide
2-{[5-Chloro-2-({(6S)-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl}amino)-4-pyrimidinyl]amino}-N-methylbenzamide

Biological Activity

[Description]:

CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).IC50 value: 2.3 nM (FAK); 120 nM (ALK cellular IC50 in 75% human plasma)Target: Dual FAK/ALKPreparation of fused bicyclic 2,4-diaminopyrimidine derivatives as a dual ALK and FAK inhibitorBy Jacobs, Martin J.; Ott, Gregory R. From PCT Int. Appl. (2013), WO 2013134353 A1 20130912.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK
Research Areas >> Cancer

[References]

[1]. From PCT Int. Appl. (2013), WO 2013134353 A1 20130912.

[2]. Salem I, et al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 2016 Mar 24;18(1):37.


[Related Small Molecules]

Brigatinib | lorlatinib | Alectinib (CH5424802) | Entrectinib | Defactinib | PND-1186 | PF-573228 | GSK2256098 | Benzol-1,2,4,5-tetramintetrahydrochlorid | TAE684(NVP-TAE684) | PF-562271 | AZD-3463 | Repotrectinib | Ensartinib | AP26113

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C30H38ClN7O3

[ Molecular Weight ]:
580.121

[ Exact Mass ]:
579.272461

[ PSA ]:
114.88000

[ LogP ]:
3.40

[ Index of Refraction ]:
1.648

[ Storage condition ]:
2-8℃

Related Compounds