Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 192 | 现货 | ||
10 mg | ¥ 313 | 现货 | ||
25 mg | ¥ 515 | 现货 | ||
50 mg | ¥ 788 | 现货 | ||
100 mg | ¥ 1,230 | 现货 | ||
500 mg | ¥ 3,130 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity |
靶点活性 | BRAF:28 nM, B-Raf (V600E):19 nM, PDGFRβ:22 nM, Raf-1:2.5 nM, VEGFR1:13 nM, VEGFR3:46 nM, VEGFR2:4.2 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]. |
别名 | 瑞戈非尼盐酸盐, BAY73-4506 hydrochloride |
分子量 | 519.28 |
分子式 | C21H16Cl2F4N4O3 |
CAS No. | 835621-07-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.6 mg/mL (10.78 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9257 mL | 9.6287 mL | 19.2574 mL | 48.1436 mL |
5 mM | 0.3851 mL | 1.9257 mL | 3.8515 mL | 9.6287 mL | |
10 mM | 0.1926 mL | 0.9629 mL | 1.9257 mL | 4.8144 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Regorafenib Hydrochloride 835621-07-3 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors PDGFR VEGFR Raf c-RET Raf kinases inhibit Inhibitor RET BAY73-4506 Hydrochloride Vascular endothelial growth factor receptor Regorafenib 瑞戈非尼盐酸盐 BAY 73-4506 BAY73-4506 hydrochloride Platelet-derived growth factor receptor inhibitor