Axitinib (AG-013736)

For research use only. Not for therapeutic Use.

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Axitinib, also known as AG013736, is an orally bioavailable tyrosine kinase inhibitor. Axitinib inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platelet-derived growth factor receptor (PDGF), thereby exerting an anti-angiogenic effect. A xitinib has received FDA (27 January 2012), EMA (13 September 2012), MHRA (3 September 2012) and TGA (26 July 2012) approval for use as a treatment for renal cell carcinoma.


Catalog Number A000203
CAS Number 319460-85-0
Synonyms

AG 013736

Molecular Formula C₂₂H₁₈N₄OS
Purity ≥95%
Target VEGFR
Solubility >19.3mg/mL in DMSO
Storage -20°C
InChI InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+
InChIKey RITAVMQDGBJQJZ-FMIVXFBMSA-N
SMILES CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4
Reference

1: Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK. Clinical
pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi:
10.1007/s40262-013-0068-3. Review. PubMed PMID: 23677771. <br />
2: Kessler ER, Bowles DW, Flaig TW, Lam ET, Jimeno A. Axitinib, a new therapeutic
option in renal cell carcinoma. Drugs Today (Barc). 2012 Oct;48(10):633-44. doi:
10.1358/dot.2012.48.10.1860768. Review. PubMed PMID: 23110259. <br />
3: Carmichael C, Lau C, Josephson DY, Pal SK. Comprehensive overview of axitinib
development in solid malignancies: focus on metastatic renal cell carcinoma. Clin
Adv Hematol Oncol. 2012 May;10(5):307-14. Review. PubMed PMID: 22706540. <br />
4: Escudier B, Gore M. Axitinib for the management of metastatic renal cell
carcinoma. Drugs R D. 2011;11(2):113-26. doi: 10.2165/11591240-000000000-00000.
Review. PubMed PMID: 21679004; PubMed Central PMCID: PMC3585900. <br />
5: Choueiri TK. Axitinib, a novel anti-angiogenic drug with promising activity in
various solid tumors. Curr Opin Investig Drugs. 2008 Jun;9(6):658-71. Review.
PubMed PMID: 18516765.

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