SKLB1002

VEGFR2

320.39

DMSO ：7 mg/mL (21.84 mM)

白色粉末

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.

6,7-二甲氧基-4-[(5-甲基-1,3,4-噻二唑-2-基)硫基]喹唑啉

C₁₃H₁₂N₄O₂S₂

1225451-84-2