SKLB1002 1225451-84-2

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Molecular Weight:

320.39 SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.


Biological Activity


SKLB1002 shows strikingly lower cytotoxicity on normal human cells L-02.
SKLB1002 significantly inhibits HUVEC proliferation, migration,
invasion, and tube formation, by inhibiting VEGF-induced phosphorylation
of VEGFR2 kinase and the downstream protein kinases including ERK, FAK,
and Src.


In the zebrafish embryos, SKLB1002 remarkably blocks the formation of
embryonic and tumor-induced Angiogenesis with no or least impact on
normal cell proliferation. In athymic mice bearing SW620 or HepG2
xenografts, SKLB1002 (100 mg/kg daily, i.p.) causes significant
inhibition of tumor growth, inhibits tumor angiogenesis and induces
tumor Apoptosis. In 4T1 and CT26 tumor model, SKLB1002
and local hyperthermia produce a synergistic antiangiogenesis,
anticancer and promotion of apoptosis efficacy.


Kinase inhibition assays


Kinase inhibition is measured by the use of radiometric assays conducted
by Kinase Profiler service. Briefly, in the presence or absence of
SKLB1002, VGFR2 (5–10 mU) is incubated in 25-μL reaction solution
containing 8 mmol/L 3-(N-morpholino)propanesulfonic acid (MOPS), pH 7.0,
0.2 mmol/L EDTA, 0.33 mg/mL myelin basic protein, 10 mmol/L Mg acetate,
and γ-[33P]ATP. After incubation for 40 minutes at room
temperature, the reaction is stopped and 10 μL of the reaction solution
is then spotted onto a P30 filtermat and washed 3 times for 5 minutes in
75 mmol/L phosphoric acid and once in methanol prior to scintillation
counting.

Method

Cell proliferation is measured using MTT assay. 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.

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Product Categories : Protein Tyrosine Kinase > VEGFR Inhibitor