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Axitinib #12961

Inquiry Info. # 12961

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    Product Information

    Product Usage Information

    Axitinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.29 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 1-1000 nM for 0.5-2 hr prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 72 hr.

    Storage

    Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 386.47 g/mol
    Purity >99%
    Molecular Formula C22H18N4OS
    CAS 319460-85-0
    Solubility Soluble in DMSO at 33mg/ml and EtOH at 1.7mg/ml.

    Background

    Axitinib is a selective inhibitor of VEGFR, PDGFR, and c-kit tyrosine kinases. Researchers performing cellular phosphorylation assays have shown that axitinib very potently inhibits VEGF-1, -2, and -3 with IC50 values of approximately 1.2 nM, 0.2 nM, and 0.1-0.3 nM, respectively. It also effectively inhibits PDGF-α (IC50 = 5.0 nM), PDGF-β (IC50 = 1.6 nM), and c-kit (IC50 = 1.7 nM) (1). Axitinib exhibits little activity against a variety of off-target protein kinases when used at 1 µM (1). It inhibits VEGF-induced endothelial cell proliferation, survival, and tube formation, as well as phosphorylation of downstream targets Akt, eNOS, and ERK1/2 in a dose-dependent manner (1). Research studies demonstrate that axitinib suppresses T cell proliferation in a dose dependent manner through G2/M mitotic arrest, while apoptosis is largely prevented though stabilization of Mcl-1 and inactivation of caspase-9 (2). Axitinib has been shown to reduce both hypoxic-induced tissue permeability and overexpression/secretion of VEGF and PDGF in HUVE and RPE cells, as well as alter junction protein expression (3).

    Alternate Names

    AG-013736; axitinib; c kit; c-kit; ckit; PDGF; PDGFR; SCF; VEGF; VEGFR

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