Regorafenib Hydrochloride
產品名稱:Regorafenib Hydrochloride
產品描述:
產品描述 | Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity |
靶點活性 | BRAF:28 nM, BRafV600E:19 nM, PDGFRβ:22 nM, Raf-1:2.5 nM, VEGFR1:13 nM, VEGFR3:46 nM, VEGFR2:4.2 nM |
體外活性 | 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. |
體內活性 | 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]. |
別名 | BAY73-4506 hydrochloride, 瑞戈非尼鹽酸鹽 |
分子量 | 519.28 |
分子式 | C21H16Cl2F4N4O3 |
CAS No. | 835621-07-3 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 5.6 mg/mL (10.78 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發,涵蓋生物科技、化學品、中間體和化工材料等領域。
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