Agerafenib(CEP-32496/RXDX-105) BRAF V600E抑制剂|CAS 1188910-76-0（53820ES）

Agerafenib (CEP-32496, RXDX-105, CEP32496, RXDX105)是可口服的BRAF V600E抑制剂，K_d为14 nM，也能抑制野生型BRAF和c-Raf，但对MAPK通路的其它关键激酶无明显亲和力，包括MEK-1/2和ERK-1/2。

参考文献

[1] Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. J Med Chem. 2012 Feb 9;55(3):1082-105.

[2] James J, et al. CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity. Mol Cancer Ther. 2012 Apr;11(4):930-41.

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