A dual inhibitor of EGFR and HER2
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AV-412

Item No. 29039

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide, 4-methylbenzenesulfonate (1:2)
CAS Number
451493-31-5
Synonyms
  • MP-412
Molecular Formula
C27H28ClFN6O • 2C7H8O3S
Formula Weight
851.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 15mg/mLDMSO: 15mg/mLDMSO:PBS (pH 7.2) (1:3): 0.25mg/mLEthanol: 0.25mg/mL
SMILES
FC1=CC=C(NC2=C(C=C(NC(C=C)=O)C(C#CC(C)(C)N3CCN(C)CC3)=C4)C4=NC=N2)C=C1Cl.CC5=CC=C(S(O)(=O)=O)C=C5.CC6=CC=C(S(O)(=O)=O)C=C6
InChi Code
InChI=1S/C27H28ClFN6O.2C7H8O3S/c1-5-25(36)33-23-16-20-24(30-17-31-26(20)32-19-6-7-22(29)21(28)15-19)14-18(23)8-9-27(2,3)35-12-10-34(4)11-13-35;2*1-6-2-4-7(5-3-6)11(8,9)10/h5-7,14-17H,1,10-13H2,2-4H3,(H,33,36)(H,30,31,32);2*2-5H,1H3,(H,8,9,10)
InChi Key
GTWJVFFZCKODEV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).1 It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 μM) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.2 It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 μM).1 It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Suzuki, T., Fujii, A., Ohya, J., et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor. Cancer Sci. 98(12), 1977-1984 (2007).

    2. Suzuki, T., Fujii, A., Ochi, H., et al. Ubiquitination and downregulation of ErbB2 and estrogen receptor-alpha by kinase inhibitor MP-412 in human breast cancer cells. J. Cell. Biochem. 112(9), 2279-2286 (2011).