WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H401980
CAS#: 1225451-84-2
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.
Hodoodo Cat#: H401980
Name: SKLB1002
CAS#: 1225451-84-2
Chemical Formula: C13H12N4O2S2
Exact Mass: 320.04
Molecular Weight: 320.390
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
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in chloroform
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 320.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
