SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
|Cell lines||HUVECs, L-02, B16-F10, HepG2, and SW620 cells.|
|Preparation method||Cell proliferation Using MTT assay to measure cell proliferation . Various cells including HUVECs, L-02, B16-F10, HepG2, and SW620 are treated with indicated concentrations of SKLB1002 for 24 hours. Vandetanib and sunitinib serve as positive controls. Each assay is replicated 3 times.|
|Incubation time||24 hours|
|Animal models||Mice bearing SW620 or HepG2 tumors|
|Formulation||35% (v/v) polyethylene glycol solution containing 5% (v/v) DMSO|
|Dosages||~100 mg/kg daily|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Related VEGFR/PDGFR Products|
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Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
|Pazopanib HCl (GW786034 )
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|Dovitinib (TKI-258) Dilactic Acid
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