CAS NO: | 835621-07-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor forVEGFR1/2/3,PDGFRβ,Kit,RETandRaf-1withIC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50of 3 nM[1]. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having an IC50of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[3]. | ||||||||||||||||
体内研究 (In Vivo) | Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 519.28 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H16Cl2F4N4O3 | ||||||||||||||||
CAS 号 | 835621-07-3 | ||||||||||||||||
中文名称 | 瑞戈非尼盐酸盐;瑞格菲尼盐酸盐 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 5.6 mg/mL(10.78 mM) H2O :< 0.1 mg/mL(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |