WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 401980
Description: SKLB1002 is a new potent VEGFR2 inhibitor, which could significantly inhibit HUVEC proliferation, migration, invasion, and tube formation. Western blot analysis was conducted, which indicated that SKLB1002 inhibited VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal-regulated kinase, focal adhesion kinase, and Src. In vivo zebrafish model experiments showed that SKLB1002 remarkably blocked the formation of intersegmental vessels in zebrafish embryos. SKLB1002 inhibits angiogenesis and may be a potential drug candidate in anticancer therapy.
MedKoo Cat#: 401980
Chemical Formula: C13H12N4O2S2
Exact Mass: 320.04017
Molecular Weight: 320.39
Elemental Analysis: C, 48.73; H, 3.78; N, 17.49; O, 9.99; S, 20.02
Synonym: SKLB1002; SKLB 1002; SKLB1002.
IUPAC/Chemical Name: 2-((6,7-dimethoxyquinazolin-4-yl)thio)-5-methyl-1,3,4-thiadiazole
InChi Key: RQVGFDBMONQTBC-UHFFFAOYSA-N
InChi Code: InChI=1S/C13H12N4O2S2/c1-7-16-17-13(20-7)21-12-8-4-10(18-2)11(19-3)5-9(8)14-6-15-12/h4-6H,1-3H3
SMILES Code: CC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1
1: Nie W, Ma XL, Sang YX, Li YL, Gao X, Xu GC, Shen GB, Shi HS, Liu XX, Wang FT, Wei YQ. Synergic antitumor effect of SKLB1002 and local hyperthermia in 4T1 and CT26. Clin Exp Med. 2012 Dec 21. [Epub ahead of print] PubMed PMID: 23263406.
2: Shen G, Li Y, Du T, Shi G, Dai L, Chen X, Zheng R, Li W, Su X, Zhang S, Wei Y, Yang S, Deng H. SKLB1002, a novel inhibitor of VEGF receptor 2 signaling, induces vascular normalization to improve systemically administered chemotherapy efficacy. Neoplasma. 2012;59(5):486-93. doi: 10.4149/neo_2012_062. PubMed PMID: 22668017.
3: Zhang S, Cao Z, Tian H, Shen G, Ma Y, Xie H, Liu Y, Zhao C, Deng S, Yang Y, Zheng R, Li W, Zhang N, Liu S, Wang W, Dai L, Shi S, Cheng L, Pan Y, Feng S, Zhao X, Deng H, Yang S, Wei Y. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res. 2011 Jul 1;17(13):4439-50. doi: 10.1158/1078-0432.CCR-10-3109. Epub 2011 May 27. PubMed PMID: 21622720.