Axitinib | VEGFR kinase inhibitor

CAS:
319460-85-0
Catalog Number:
10-2118
Activity:
VEGFR kinase inhibitor
Chemical Name:
N-Methyl-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide
Molecular Weight:
386.47
Molecular Formula:
C22H18N4OS
Solubility:
Soluble in DMSO (up to 30 mg/ml)
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
10 mg$40.00
50 mg$110.00

Axitinib (319460-85-0) is a potent inhibitor of VEGFR-2, -3, and -1, IC50 = 0.2, 0.1-0.3, and 1.2 nM respectively1 displaying minimal activity against a panel of ~100 protein kinases. Inhibits angiogenesis and vascular permeability.2 Also inhibits BCR-ABL1 (T315I) with high potency, Ki = 149 pM for autophosphorylated ABL1 (T315I).3 Inhibits proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Clinically useful anticancer agent.4 Axitinib downregulated STAT3 expression leading to a significant decrease in immunosuppressive myeloid-derived suppressor cells.5 It increased CD8+ T cells, reduced myeloid-derived suppressor cells, and suppressed the expressions of proinflammatory cytokines in B116F1 melanoma cells.6

References/Citations:

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 1,2,3; Cancer Res., 14 7272
2) Ma and Waxman (2008), Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib; Mol. Cancer Ther., 7 79
3) Pemovska et al. (2015), Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation; Nature, 519 102
4) Rixe et al. (2007), Axitinib treatment in patients with cytokine-refractory metastatic renal-cell cancer; a phase II study; Lancet Oncol., 8 975
5) Yuan et al. (2014), Axitinib augments antitumor activity in renal cell carcinoma via STAT3-dependent reversal of myeloid-derived suppressor cell accumulation; Biomed.Pharmacother. 68 751
6) Zhang et al. (2014), Axitinib, a selective inhibitor of vascular endothelial growth factor receptor, exerts an anticancer effect in melanoma through promoting antitumor immunity; Anticancer Drugs 25 204

CAS:
319460-85-0
Catalog Number:
10-2118
Activity:
VEGFR kinase inhibitor
Chemical Name:
N-Methyl-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide
Molecular Weight:
386.47
Molecular Formula:
C22H18N4OS
Solubility:
Soluble in DMSO (up to 30 mg/ml)
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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