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    InvivoChem Cat #: V0496
    CAS #: 883986-34-3Purity ≥98%

    Description: AZD2932 (AZD-2932), a new quinazoline ether, is a novel, potent, high affinity and mutil-targeted tyrosine kinase inhibitor with potential anticancer activity. It inhibits VEGFR-2, PDGFRβ, Flt-3, and c-Kit with IC50 values of 8 nM, 4 nM, 7 nM, and 9 nM, respectively. AZD-2932 is also active on c-Kit and FLT3 with good selectivity on a panel of kinases. The pharmacokinetic behavior and the preclinical antitumor activity in nude mice bearing C6 rat glial tumors indicate that 31 has the potential to become an antiangiogenic agent in the clinic.

    References: Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.

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    Molecular Weight (MW)447.49
    CAS No.883986-34-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (198.9 mM)
    Water: <1 mg/mL
    Ethanol: 5 mg/mL warmed (11.2 mM)
    Other infoChemical Name: 2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetamide
    InChi Code: InChI=1S/C24H25N5O4/c1-15(2)29-13-17(12-27-29)28-23(30)9-16-5-7-18(8-6-16)33-24-19-10-21(31-3)22(32-4)11-20(19)25-14-26-24/h5-8,10-15H,9H2,1-4H3,(H,28,30)
    SMILES Code: O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)C=C2
    SynonymsAZD-2932; AZD2932; AZD 2932

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    In Vitro

    In vitro activity: AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). AZD2932 inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. AZD2932 does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50, 137 μM).

    Kinase Assay: AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.

    In VivoIn C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in significant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). AZD2932 (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of AZD2932 results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing.
    Animal modelC6 rat glial tumor model
    Formulation & Dosage50 and 12.5 mg/kg; oral
    ReferencesBioorg Med Chem Lett. 2012 Jan 1;22(1):262-6

    These protocols are for reference only. InvivoChem does not independently validate these methods.



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