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Regorafenib
CAS No. : 755037-03-7
MCE 国际站：Regorafenib
产品活性：Regorafenib (BAY 73-4506) 是一种口服有效的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂，抑制 VEGFR1/2/3，PDGFRβ，Kit，RET 和 Raf-1 的 IC50 分别为 13/4.2/46，22，7，1.5 和 2.5 nM。Regorafenib 显示出非常强的抗肿瘤和抗血管生成活性。
研究领域：Protein Tyrosine Kinase/RTK | Autophagy | MAPK/ERK Pathway
作用靶点：VEGFR | Autophagy | PDGFR | Raf | RET | c-Kit | FGFR | Tie
In Vitro: Regorafenib (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells.
Regorafenib (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.
Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.
In Vivo: Regorafenib (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
Regorafenib (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model.
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