产品信息
抗原名称
DDR2；EPHA3；Axl；Mer；VEGFR3 (FLT4)
商品描述
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.
分子量
629.68
纯度
98%
可溶性
DMSO : ≥ 32 mg/mL (50.82 mM)
外观
Off-white solid
In vitro(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.
In vivo(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.
背景
分子式
C33H29F2N5O4S
CAS号
1123837-84-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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