SKLB1002 Chemical Properties

Melting point:

193 °C

Boiling point:

522.4±60.0 °C(Predicted)

Density 

1.45±0.1 g/cm3(Predicted)

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

insoluble in H2O; ≥5 mg/mL in EtOH with gentle warming and ultrasonic; ≥8 mg/mL in DMSO

form 

powder to crystal

pka

-0.14±0.30(Predicted)

color 

White to Light yellow

Safety Information

HS Code 

2934.99.3900

SKLB1002 Usage And Synthesis

Uses

SKLB1002 is a potent vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor that inhibits angiogenesis and tumor growth in vivo.

Biological Activity

sklb1002 is a potent inhibitor of vegf receptor 2 with ic50 value of 32 nm [1].vegf receptor 2 (vegfr2) is a major receptor for vascular endothelial growth factor (vegf) and plays an important role in angiogenesis and vegf-stimulated proliferation, migration, and sprouting of cultured endothelial cells [1].sklb1002 is a potent vegfr2 inhibitor. in human umbilical vein endothelial cells (huvec), sklb1002 significantly inhibited vegf-induced huvec proliferation with ic50 value of 11.9 μm. also, sklb1002 inhibited huvec migration, invasion and tube formation in a dose-dependent way. sklb1002 (10 μm) significantly inhibited vegf-induced phosphorylation of vegfr2, erk, src and fak [1].in zebrafish embryos, sklb1002 (2.5 μm) significantly inhibited the growth of intersegmental vessels. in mice bearing sw620 or hepg2 xenografts, sklb1002 (100 mg/kg) significantly inhibited tumor volume and inhibited tumor growth by 60%. also, sklb1002 reduced the microvessel density [1]. in mice with 4t1 tumor, sklb1002 significantly reduced the tumor vessel density [2].

target

VEGFR2

References

[1]. zhang s, cao z, tian h, et al. sklb1002, a novel potent inhibitor of vegf receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. clin cancer res, 2011, 17(13): 4439-4450.
[2]. shen g, li y, du t, et al. sklb1002, a novel inhibitor of vegf receptor 2 signaling, induces vascular normalization to improve systemically administered chemotherapy efficacy. neoplasma, 2012, 59(5): 486-493.

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