An inhibitor of Her2/Neu tyrosine kinase activity
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AG-825

Item No. 10010243

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[3-[(2-benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide
CAS Number
149092-50-2
Synonyms
  • Tyrphostin AG-825
Molecular Formula
C19H15N3O3S2
Formula Weight
397.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO: PBS (pH 7.2)(1:3): 0.1 mg/mlEthanol: 0.2 mg/ml
λmax
225, 361 nm
SMILES
OC(C(OC)=CC(C=C(C#N)C(N)=O)=C1)=C1CSC2=NC3=CC=CC=C3S2
InChi Code
InChI=1S/C19H15N3O3S2/c1-25-15-8-11(6-12(9-20)18(21)24)7-13(17(15)23)10-26-19-22-14-4-2-3-5-16(14)27-19/h2-8,23H,10H2,1H3,(H2,21,24)
InChi Key
KXDONFLNGBQLTN-UHFFFAOYSA-N
Origin
Synthetic
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $99

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    10 mg

    $168

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    25 mg

    $380

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    Product Description

    AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.1 However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.1 Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Osherov, N., Gazit, A., Gilon, C., et al. Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins. The Journal of Biological Chemisty 268(15), 11134-11142 (1993).

    2. Murillo, H., Schmidt, L.J., and Tindall, D.J. Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-2. Cancer Res. 61, 7408-7412 (2001).