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产品价格:电议      采购度:1593      原产地:美洲
发布时间:2021/7/24 3:55:03 所属地区:上海 上海市
简要描述:
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, nM,46 nM,22 nM,7 nM, nM 和 nM。
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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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更新时间:2024/1/2 10:14:41
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