SKLB610 is a VEGFR inhibitor that potently suppresses human tumor angiogenesis. SKLB610 inhibited angiogenesis-related tyrosine kinase VEGFR2, fibroblast growth factor receptor 2 (FGFR2) and platelet-derived growth factor receptor (PDGFR) at rate of 97%, 65% and 55%, respectively, at concentration of 10μM in biochemical kinase assays. SKLB610 exhibited its antitumor activity as a multi-targeted inhibitor with more potent inhibition of VEGFR2 activity. Its potential to be a candidate of anticancer agent is worth being further investigated.
Chemical Formula: C21H16F3N3O3
Exact Mass: 415.11438
Molecular Weight: 415.36525
Elemental Analysis: C, 60.72; H, 3.88; F, 13.72; N, 10.12; O, 11.56
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 DMSO, not in water
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
SKLB610 has a selective inhibition of VEGF-induced proliferation with an IC50 value of 2.2μM. In HUVECs, SKLB610 shows selectivity of 2-fold for inhibition of VEGF-induced proliferation versus bFGF-induced proliferation with an IC50 value of 4.7μM. In HUVECs, SKLB610 blocks VEGF stimulated phosphorylation of VEGFR2 in a dose dependent manner after SKLB610 treatment. SKLB610 significant inhibits HUVECs capillary tube formation in a concentration-dependent manner. SKLB610 inhibits the formation of vessel-like structures at 2.5 μM.
SKLB-610 inhibits tumor xenograft model growth of human non-smallcell lung cancer model (A549) and human colon cancer model (HCT116) and is well tolerated. After 30 days treatment, SKLB610 exhibited a significantly antitumor activity in inhibiting tumor progress compared with control. The inhibition rate of tumor volume in SKLB610-treated groups is 70.2% (50 mg/kg) for A549 and 77.1% (50 mg/kg) for HCT116 . The retention times of SKLB610 and the internal standard are 5.6 and 8.1 min, respectively. The quantification limit is 67 ng/mL. The calibration curves are linear over a concentration range of 0.1–50 µg/mL.
Huang Y, Luo X, You X, Xia Y, Song X, Yu L. The preparation and evaluation of water-soluble SKLB610 nanosuspensions with improved bioavailability. AAPS PharmSciTech. 2013 Sep;14(3):1236-43. doi: 10.1208/s12249-013-0005-7. Epub 2013 Aug 10. PubMed PMID: 23934433; PubMed Central PMCID: PMC3755164.
Luo X, Li S, Xie Y, He J, Li J, Lin H, Wang N, Yang S, Zhao Y, Yu L, Song X. Pharmacokinetic studies of a novel multikinase inhibitor for treating cancer by HPLC-UV. J Chromatogr Sci. 2013 Jan;51(1):17-20. doi: 10.1093/chromsci/bms098. Epub 2012 Jun 17. PubMed PMID: 22710664.
Cao ZX, Zheng RL, Lin HJ, Luo SD, Zhou Y, Xu YZ, Zeng XX, Wang Z, Zhou LN, Mao YQ, Yang L, Wei YQ, Yu LT, Yang SY, Zhao YL. SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol Biochem. 2011;27(5):565-74. doi: 10.1159/000329978. Epub 2011 Jun 15. PubMed PMID: 21691074.
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