Protein Inhibitors - Axitinib (CAS: 319460-85-0)

Axitinib (CAS: 319460-85-0)

Catalog #：EBC51020

Biological Activity

Synonyms

AG 013736

Chemical Name

N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide

Application

Axitinib is a selective inhibitor of VEGFR, PDGFR, and c-kit tyrosine kinases.

CAS Number

319460-85-0

Purity

≥99.0%

Molecular Weight

386.47

Molecular Formula

C22H18N4OS

SMILES

CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4

Target & IC50

PDGF-α: IC50 = 5.0 nM
PDGF-β: IC50 = 1.6 nM
VEGFR1/FLT1: IC50 = 0.1 nM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	2.5875 ml	12.9376 ml	25.8752 ml
5 mM	0.5175 ml	2.5875 ml	5.1750 ml
10 mM	0.2588 ml	1.2938 ml	2.5875 ml
50 mM	0.0518 ml	0.2588 ml	0.5175 ml

Solubility
DMSO: 26 mg/mL (67.28 mM)

Product Description

Axitinib is a selective inhibitor of VEGFR, PDGFR, and c-kit tyrosine kinases. Axitinib inhibited the phosphorylation of VEGFR-1, 2 and 3 with IC50 values of 1.2 nM, 0.2 nM and 0.1 to 0.3 nM in cells, respectively. In HUVEC cells, Axitinib inhibited VEGFR-2 stimulated cell survival with about 1000-fold selectivity against FGFR-1. Axitinib also significantly suppressed the phosphorylation of VEGF downstream signaling molecules including Akt, eNOS and ERK1/2. Besides that, axitinib inhibited VEGFR-2 phosphorylation with EC50 value of 0.49 nM in vivo. It delayed tumore growth of human xenograft tumors in mice such as M24met, HCT-116 and SN12C.