瑞戈非尼盐酸盐 T8402

Product Introduction
Bioactivity


英文名: Regorafenib Hydrochloride

描述: Regorafenib Hydrochloride (BAY73-4506 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。

体外活性: 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.

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 5.6 mg/mL (10.78 mM)


关键字: Raf | Regorafenib Hydrochloride | PDGFR | Raf kinases | inhibit | Inhibitor | RET | BAY73-4506 Hydrochloride | Vascular endothelial growth factor receptor | Regorafenib | Autophagy | VEGFR | BAY 73-4506 | Platelet-derived growth factor receptor

相关产品: ZM 336372 | LY3009120 | SB-590885 | Regorafenib | Lifirafenib | B-Raf IN 15 | Effusanin A | K-Ras-IN-1 | Sorafenib-d3 | Zabofloxacin hydrochloride

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途