Sulfatinib (HMPL-012) 是一种有效且高度选择性的针对 VEGFR1/2/3，FGFR1和 CSF1R 的酪氨酸激酶抑制剂，IC₅₀ 值在1 到 24 nM之间。

Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s of in a range of 1 to 24 nM.

Solid

VEGFR1 VEGFR2

Sulfatinib inhibits VEGFR1, 2, and 3, FGFR1 and CSF1R kinases with IC50s in a range of 1 to 24 nM, and it strongly blocks VEGF induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1 stimulated CSF1R phosphorylation in RAW264.7 cells with IC50 of 2 and 79 nM, respectively. Sulfatinib also attenuates VEGF or FGF stimulated HUVEC cells proliferation with IC50< 50 nM. Also, it is a hERG inhibitor with IC50 of 6.8 μM in CHO cell. has not independently confirmed the accuracy of these methods. They are for reference only.

In animal studies, a single oral dosing of Sulfatinib inhibits VEGF stimulated VEGFR2 phosphorylation in lung tissues of nude mice in an exposure-dependent manner. Furthermore, elevation of FGF23 levels in plasma 24 hours post dosing suggests suppression of FGFR signaling. Sulfatinib demonstrates potent tumor growth inhibition in multiple human xenograft models and decreases CD31 expression remarkably, suggesting strong inhibition on angiogenesis through VEGFR and FGFR signaling. In a syngeneic murine colon cancer model CT-26, Sulfatinib demonstrates moderate tumor growth inhibition after single agent treatment. After oral dosing of 10 mg/kg, the AUC and C max are 397 ng/mL and 138ng/mL in the mouse, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.

In Vitro: DMSO : ≥ 100 mg/mL (208.08 mM)配制储备液