KG 5 是一种具有口服活性的双重 PDGFRβ 和 B-Raf 别构抑制剂。 KG 5 还抑制 Flt3、KIT 和 c-Raf。 KG 5 具有抗癌、抗血管生成活性。
PDGFRβ and B-Raf allosteric inhibitor. Also inhibits c-Raf, FLT3 and KIT. Disrupts blood vessel formation in zebrafish embryos and inhibits angiogenesis in a mouse angiogenesis model. Inhibits growth of renal and pancreatic tumors in mice. Also arrests cells in prometaphase. Orally available.
Murphy et al (2010) Disruption of angiogenesis and tumor growth with an orally active drug that stabilizes the inactive state of PDGFRbeta/B-RAF. Proc.Natl.Acad.Sci.U.S.A. 107 4299 PMID:20154271 |Mielgo et al (2011) A MEK-independent role for CRAF in mitosis and tumor progression. Nat.Med. 17 PMID:22081024
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