DC Chemicals Supply: SKLB1002, Cas: 1225451-84-2 ,Cat No. DC7501, Purity>98%, In stock.
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SKLB1002|cas 1225451-84-2, Synonym name: SKLB 1002; SKLB-1002, Chemical name: 2-((6,7-dimethoxyquinazolin-4-yl)thio)-5-methyl-1,3,4-thiadiazole, Molecule weight: 320.39, Molecule Formula: C13H12N4O2S2
SKLB1002 is a novel and potent VEGFR-2 inhibitor with an IC50 value of 32 nM.
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 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]
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