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SKLB1002

Catalog No.
B1305
VEGFR2 inhibitor,potent and ATP-competitve
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$83.00
In stock
5mg
$75.00
In stock
10mg
$138.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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].

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt320.39
Cas No.1225451-84-2
FormulaC13H12N4O2S2
Solubilityinsoluble in H2O; ≥5 mg/mL in EtOH with gentle warming and ultrasonic; ≥8 mg/mL in DMSO
Chemical Name2-(6,7-dimethoxyquinazolin-4-yl)sulfanyl-5-methyl-1,3,4-thiadiazole
SDFDownload SDF
Canonical SMILESCC1=NN=C(S1)SC2=NC=NC3=CC(=C(C=C32)OC)OC
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description SKLB1002 is a potent inhibitor of VEGF receptor 2 (VEGFR2) with IC50 value of 32 nM.
Targets VEGFR2          
IC50 32 nM          

Quality Control

Chemical structure

SKLB1002