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Product IntroductionBioactivity英文名: Regorafenib Hydrochloride描述: Regorafenib Hydrochloride (BAY73-4506 hydrochloride) 是一种
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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
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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