Sulfatinib-(HMPL-012)-FGFR-Inhibitor-MedChemExpress

Sulfatinib

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[1]. After oral dosing of 10 mg/kg, the AUC and C max

are 397 ng/mL and 138ng/mL in the mouse, respectively[1].

PROTOCOL

Kinase Assay [2]The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. The testing system contains 300 ng/mL of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound

(Sulfatinib) at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition

proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5 μL of stop solution is added

to stop the reaction[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration [2]The phamacokinetics of Sulfatinib are studied with male ICR mice (n=6 for each group, weight 20-30g) after a single intraveneous and oral dosing at 2.5 and 10mg/kg, respectively. For i.v. dosing formulation, Sulfatinib is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

REFERENCES

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

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Caution: Product has not been fully validated for medical applications. For research use only.

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