319460-85-0 Axitinib AKSci A819
 
 
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  A819    
Axitinib
, 98% (HPLC)
 
N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide
Inlyta




IDENTITY
CAS Number:319460-85-0
MDL Number:MFCD09837898
MF:C22H18N4OS
MW:386.47
SPECIFICATIONS & PROPERTIES
Purity:98% (HPLC)
Physical Form:White to tan powder
Melting Point:211-214°C
Long-Term Storage:Store long-term at -20°C

BIOLOGICAL INFO
Solubility:DMSO: 42mg/mL; H2O: <1mg/mL; EtOH: <1mg/mL
Application(s):Inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor recep
Form:Free base

REVIEW

 The vascular endothelial growth factor receptor (VEGFR), a signal protein, is responsible for the origination and progression of various tumours. VEGFR-1 plays a major role in the growth of new blood vessels from the old blood vessels (angiogenesis) and tumour growth. VEGFR-2 plays an important role in the endothelial cell proliferation, migration and survival, and angiogenesis. VEGFR-3 is involved in the formation of new lymphatic vessels from already existing lymphatic vessels (lymphangiogenesis). Axitinib has the ability to inhibit VEGFR-1, 2 and 3 selectively. It binds to the receptors of the VEGF and inhibits it, thereby preventing the formation of new blood vessels.

REFERENCES
[1]Hu-Lowe et al (2008) Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2 and 3. Clin.Cancer Res. 14 7272. PMID: 19010843.
[2] Ma and Waxman (2008) Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib. Mol.Cancer Ther. 7 79. PMID: 18202011.
[3] Wilmes LJ, Pallavicini MG, Fleming LM, Gibbs J, Wang D, Li KL, Partridge SC, Henry RG, Shalinsky DR, Hu-Lowe D, Park JW, McShane TM, Lu Y, Brasch RC, Hylton NM. (2007) AG-013736, a novel inhibitor of VEGF receptor tyrosine kinases, inhibits breast cancer growth and decreases vascular permeability as detected by dynamic contrast-enhanced magnetic resonance imaging. Magn Reson Imaging 25(3):319-27
[4] Rini B, Rixe O, Bukowski R, Michaelson MD, Wilding G, Hudes G, Bolte O, Steinfeldt H, Reich SD, Motzer R. (2005) AG-013736, a multi-target tyrosine kinase receptor inhibitor, demonstrates anti-tumor activity in a Phase 2 study of cytokine-refractory, metastatic renal cell cancer (RCC). ASCO Proceedings Abstract 4509.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H302; H410

Precautionary Statements
P264; P270; P273; P301+P312; P330; P391; P501


Current as of June 24, 2019


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CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


PubChem