Catalog No.S7258

SKLB1002 Chemical Structure

Molecular Weight(MW): 320.39

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

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Biological Activity

Description SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
VEGFR2 [1]
32 nM
In vitro

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. [1]

In vivo 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. [1] In 4T1 and CT26 tumor model, SKLB1002 and local hyperthermia produce a synergistic antiangiogenesis, anticancer and promotion of apoptosis efficacy. [2]


Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: HUVECs, L-02, B16-F10, HepG2, and SW620 cells.
  • Concentrations: ~40 μM
  • Incubation Time: 24 hours
  • 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.
    (Only for Reference)
Animal Research:[1]
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  • 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
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 7 mg/mL (21.84 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 320.39


CAS No. 1225451-84-2
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID