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Regorafenib monohydrate

CAS No. : 1019206-88-2

MCE 站：Regorafenib monohydrate

产品活性：Regorafenib monohydrate (BAY 73-4506 monohydrate) 是一种多靶点抑制剂，对VEGFR1/2/3，PDGFRβ，Kit，RET 和 Raf-1 的 IC₅₀ 分别为 13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM 和 2.5 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy  |  MAPK/ERK Pathway

作用靶点：VEGFR  |  Autophagy  |  PDGFR  |  Raf  |  RET

In Vitro: Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC₅₀ of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC₅₀ of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC₅₀ of 3 nM. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having an IC₅₀ of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.

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.

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