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    SKLB1002 (SKLB-1002; SKLB 1002)
    SKLB1002 (SKLB-1002; SKLB 1002)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0500
    CAS #: 1225451-84-2Purity ≥98%

    Description: SKLB1002 (SKLB-1002; SKLB 1002) is a novel, potent and ATP-competitive VEGFR2 (VEGF receptor 2) inhibitor with potential antitumor activity. It inhibits VEGFR2 with an  IC50 of 32 nM. It exhibits excellent anti-proliferative activity in vitro and high in vivo antitumor efficacy in mice bearing SW620 or HepG2 tumors. 

    References: Clin Cancer Res. 2011 Jul 1;17(13):4439-50; Clin Exp Med. 2014 May;14(2):203-13. 

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    Molecular Weight (MW)320.39
    FormulaC13H12N4O2S2
    CAS No.1225451-84-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 7 mg/mL (21.8 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/mL
    SMILESCC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1
    SynonymsSKLB 1002; SKLB1002; SKLB-1002; 2-((6,7-dimethoxyquinazolin-4-yl)thio)-5-methyl-1,3,4-thiadiazole 

    InChi Key: RQVGFDBMONQTBC-UHFFFAOYSA-N

    InChi Code: InChI=1S/C13H12N4O2S2/c1-7-16-17-13(20-7)21-12-8-4-10(18-2)11(19-3)5-9(8)14-6-15-12/h4-6H,1-3H3

    SMILES Code: CC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1


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    In Vitro

    In vitro 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.


    Kinase Assay: 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 Assay: 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.

    In VivoIn 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.
    Animal modelMice bearing SW620 or HepG2 tumors.
    Formulation & Dosage Dissolved in 35% (v/v) polyethylene glycol solution containing 5% (v/v) DMSO; 100 mg/kg; i.p.
    References

    Clin Cancer Res. 2011 Jul 1;17(13):4439-50; Clin Exp Med. 2014 May;14(2):203-13. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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