Sitravatinib,1123837-84-2

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产品名称：Sitravatinib

产品别名：见爱必信官网

英文别名：MG-516

靶点：DDR2 ,EPHA3 ,Axl ,Mer ,VEGFR3 (FLT4)

CAS：1123837-84-2

纯度：见爱必信官网

外观：见爱必信官网

保存方法：见爱必信官网

描述：Sitravatinib (MGCD516; MG516) is an orally bioavailable, receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT , FLT3, DDR2, DDR1, TRKA, TRKB, respectively[1].

溶解性：DMSO: ≥ 32 mg/mL

体外研究：

MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.

体内研究：Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.

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