Axitinib Inhibitor CAS No. 319460-85-0

Cat. No.	Name	Size	Price	Add Cart
KI0443	Axitinib	50 mg	$112
KI0443	Axitinib	100 mg	$192

Chemical Characteristic

Product Name	Axitinib
Synonyms	AG13736, AG-013736, Inlyta
CAS No.	319460-85-0
Molecular Weight	386.469
Formula	C₂₂H₁₈N₄OS
Chemical Name	N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide
Smiles	C(=O)(c1c(cccc1)Sc1ccc2c(n[nH]c2c1)/C=C/c1ccccn1)NC
Chemical Structure
Documents	COA HPLC MS

Biological activities

Axitinib is a potent and selective inhibitor of VEGF receptor tyrosine kinase (RTK) 1, 2, and 3. Axitinib inhibits cellular autophosphorylation of VEGF receptors (VEGFR) with picomolar IC50 values. IC50s of axitinib for VEGFR-2 and VEGFR-3 are 0.2 and 0.1 to 0.3 nM, respectively. Axitinib blocks not only VEGF-mediated endothelial cell survival but also tube formation, as well as downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase. Axitinib has little inhibition against ??ff-target??protein kinases. At a concentration of 1 μM, axitinib prevents only five protein kinases including Abl, Aurora-2, Arg, AMPK, Axl, and MST2 by ??0%. Axitinib inhibits VEGF-mediated endothelial cell survival, migration, and tube formation. Acute axitinib treatment rapidly and significantly decreases retinal vascular VEGFR-2 phosphorylation.^[1] Following twice daily oral administration, axitinib produces consistent and dose-dependent antitumor efficacy that is associated with blocking VEGFR-2 phosphorylation, vascular permeability, angiogenesis, and concomitant induction of tumor cell apoptosis. A single oral dose of axitinib (100 mg/kg) markedly suppresses murine VEGFR-2 phosphorylation for up to 7 hours compared with control tumors. Axitinib produces growth delay regardless of initial tumor size, model type, or implant site in a dose-dependent manner. Importantly, axitinib reveals primary tumor inhibition and distant metastasis control in orthotopically implanted tumors such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). The AED_{50 of axitinib is 8.8 mg/kg twice daily. Based on C_{min (trough concentration), the estimated unbound C_{eff of axitinib is 0.28 nM. In the MDA-MB-435/HAL-luc model, axitinib (30 mg/kg) and docetaxel (5 mg/kg; 25% of murine maximally tolerated dose) produce a robust tumor growth.^[1]}}}

Protocols

Axitinib is dissolved in 10 mM DMSO. ^[1]

References

[1] Hu-Lowe DD, et al. 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. Clin Cancer Res. 2008, 14(22): 7272-7283.

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