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PDGFR&FGFR

SKLB610 (1125780-41-7)

SKLB610 is a VEGFR inhibitor that potently suppresses human tumor angiogenesis.  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.

Not Intended for Therapeutic Use. For research use only.

CAS: 1125780-41-7 Category

SKLB610 (1125780-41-7) Description:

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. In vitro, SKLB610 showed more selective inhibition of VEGF-stimulated human umbilical vein endothelial cells (HUVECs) proliferation, and this proliferation inhibitory effect was associated with decreased phosphorylation of VEGFR2 and p42/44 mitogen-activated protein kinase (p42/44 MAPK).Antiangiogenic evaluation showed that SKLB610 inhibited the HUVECs capillary-tube formation on Matrigel in vitro and the sub-intestinal vein formation of zebrafish in vivo. Moreover, SKLB610 inhibited a panel of human cancer cells proliferation in a concentration-dependent manner and human non-small cell lung cancer cell line A549 and human colorectal cancer cell line HCT116 were most sensitive to SKLB610 treatment. In vivo, chronic intraperitoneally administration of SKLB610 at dose of 50mg/kg/d resulted in significant inhibition in the growth of established human A549 and HCT116 tumor xenografts in nude mice without exhibit toxicity. Histological analysis showed significant reductions in intratumoral microvessel density (CD31 staining) of 43-55% relative to controls depending on the specific tumor xenografts. In conclusion, the present study demonstrated that 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.

SKLB610 (1125780-41-7) Specifications:

Product Name SKLB610
Synonym SKLB610; SKLB 610; SKLB-610.
Chemical Name N-methyl-4-(4-(3-(trifluoromethyl)benzamido)phenoxy)picolinamide
Purity ≥98% (HPLC)
CAS Number 1125780-41-7
Molecular Formula C21H16F3N3O3
Molecular Weight 415.372 g/mol
Monoisotopic Mass 415.114 g/mol
MDL number N/A
InChIKey WACDHHMEVMSODJ-UHFFFAOYSA-N
InChi Code InChI=1S/C21H16F3N3O3/c1-25-20(29)18-12-17(9-10-26-18)30-16-7-5-15(6-8-16)27-19(28)13-3-2-4-14(11-13)21(22,23)24/h2-12H,1H3,(H,25,29)(H,27,28)
SMILES O=C(NC)C1=NC=CC(OC2=CC=C(NC(C3=CC=CC(C(F)(F)F)=C3)=O)C=C2)=C1
Form Powder
Color N/A
Solubility  ≥20.75mg/mL in DMSO
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application VEGFR inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. 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.

[2]. SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. 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. Cell Physiol Biochem. 2011;27(5):565-74. doi: 10.1159/000329978. Epub 2011 Jun 15. PMID: 21691074

[3]. The preparation and evaluation of water-soluble SKLB610 nanosuspensions with improved bioavailability. Huang Y, Luo X, You X, Xia Y, Song X, Yu L. AAPS PharmSciTech. 2013 Sep;14(3):1236-43. doi: 10.1208/s12249-013-0005-7. Epub 2013 Aug 10. PMID: 23934433

[4]. 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.

[5]. 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.

1 review for SKLB610 (1125780-41-7)

  1. Cofttek

    Never had such good experience before,The SKLB610 (1125780-41-7) is high purity,also customer service is pretty nice !gotta try!!

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