Description
Regorafenib (BAY 73-4506) can inhibit c-KIT, VEGFR2 and B-Raf with IC50 of 17 nM, 40 nM and 69 nM.
Storage
2 years at -20centigrade Powder
Targets
VEGFR2, B-Raf, c-KIT
Molecular Formula
C21H15ClF4N4O3
Chemical Name
1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
Solubility
DMSO 97 mg/mL Water
In vitro
As a multikinase inhibitor of of angiogenic, stromal and oncogenic receptor tyrosine kinases, Regorafenib (BAY 73-4506) can inhibit c-KIT, VEGFR-2, B-Raf with IC50 of 17 nM, 40 nM and 69 nM. Regorafenib (BAY 73-4506) also inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-beta and fibroblast growth factor receptor 1) and the mutant RET.
In vivo
(1)Regorafenib showed an acceptable safety profile and preliminary evidence of antitumor activity in patients with solid tumors. (2)Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts.A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qdx5 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. (3) Regorafenib showed tolerability and antitumour activity in patients with metastatic CRC. (4) Regorafenib has significant activity in patients with advanced GIST (Metastatic GI stromal tumor) after failure of both imatinib and sunitinib.
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