Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
Description | Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity |
Targets&IC50 | Raf-1:2.5 nM, PDGFRβ:22 nM, BRafV600E:19 nM, BRAF:28 nM, VEGFR1:13 nM, VEGFR2:4.2 nM, VEGFR3:46 nM |
In vitro | 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. |
In vivo | 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]. |
Synonyms | BAY73-4506 hydrochloride, 瑞戈非尼盐酸盐 |
Molecular Weight | 519.28 |
Formula | C21H16Cl2F4N4O3 |
CAS No. | 835621-07-3 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 5.6 mg/mL (10.78 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Regorafenib Hydrochloride 835621-07-3 MAPK信号通路 蛋白酪氨酸激酶 凋亡 血管生成 自噬 Autophagy c-RET PDGFR Raf VEGFR Raf kinases inhibit Inhibitor RET Vascular endothelial growth factor receptor Regorafenib BAY73-4506 hydrochloride BAY 73-4506 Platelet-derived growth factor receptor inhibitor