RegoRafenib Hydrochloride 是一种新型口服多激酶抑制剂，可抑制血管生成、基质和致癌受体酪氨酸激酶，具有强大的临床前抗肿瘤活性。它靶向作用于VEGFR1/2/3、PDGFRβ、Kit、RET和Raf-1，IC50值分别为 13/4.2/46、22、7、1.5 和 2.5 nM。

Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

Regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-β and fibroblast growth factor receptor 1) and the mutant oncogenic kinases KIT, RET and B-RAF.

Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts.?In a daily (qd)×4 dosing study, the pharmacodynamic effects persisted for 48 hr after the last dosing and correlated with tumor growth inhibition (TGI).?A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qd×5 dosing at 10 and 30 mg/kg.?Regorafenib exhibited potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages observed in breast MDA-MB-231 and renal 786-O carcinoma models.?Pharmacodynamic analyses of the breast model revealed strong reduction in staining of proliferation marker Ki-67 and phosphorylated extracellular regulated kinases 1/2[1].

835621-07-3

C21H16Cl2F4N4O3

519.28

BAY73-4506 hydrochloride;瑞戈非尼盐酸盐

DMSO:5.6 mg/mL (10.78 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years