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].

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].

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].

519.28

Solid

C₂₁H₁₆Cl₂F₄N₄O₃

835621-07-3

瑞戈非尼盐酸盐；瑞格菲尼盐酸盐

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : ≥ 5.6 mg/mL(10.78 mM)

H₂O :< 0.1 mg/mL(insoluble)

*"≥" means soluble, but saturation unknown.

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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。