A tyrphostin that inhibits EGFR and HER2
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AG-528

Item No. 29666

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αE-[(3,4-dihydroxyphenyl)methylene]-2,3-dihydro-β-oxo-1H-indole-1-propanenitrile
CAS Number
133550-49-9
Synonyms
  • Tyrphostin AG-528
Molecular Formula
C18H14N2O3
Formula Weight
306.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
248, 363 nm
SMILES
O=C(/C(C#N)=C/C1=CC(O)=C(O)C=C1)N2CCC3=CC=CC=C32
InChi Code
InChI=1S/C18H14N2O3/c19-11-14(9-12-5-6-16(21)17(22)10-12)18(23)20-8-7-13-3-1-2-4-15(13)20/h1-6,9-10,21-22H,7-8H2/b14-9+
InChi Key
MYKCTDWWIWGLHW-NTEUORMPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $61

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    50 mg

    $273

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    100 mg

    $484

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    250 mg

    $1,060

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    Product Description

    AG-528 is a tyrphostin that inhibits EGFR and HER2 (IC50s = 12 and 4.9 μM, respectively, for inhibition of autophosphorylation).1 It also inhibits pantothenate kinase 3 (PanK3; IC50 = 3 μM).2 AG-528 inhibits EGF-dependent proliferation of HER14 cells (IC50 = 25 μM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gazit, A., Osherov, N., Posner, I., et al. Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J. Med. Chem. 34(6), 1896-1907 (1991).

    2. Leonardi, R., Zhang, Y.-M., Yun, M.-K., et al. Modulation of pantothenate kinase 3 activity by small molecules that interact with the substrate/allosteric regulatory domain. Chem. Biol. 17(8), 892-902 (2010).