SKLB1002 Property

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

HS Code 

2934.99.3900

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

SKLB1002 Chemical Properties,Usage,Production

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.