An inhibitor of Bcr-Abl and c-Abl
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AG957

Item No. 17259

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(2,5-dihydroxyphenyl)methyl]amino]-benzoic acid, methyl ester
CAS Number
140674-76-6
Synonyms
  • NSC 654705
  • Tyrphostin AG957
Molecular Formula
C15H15NO4
Formula Weight
273.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 5 mg/ml
λmax
225, 308 nm
SMILES
OC1=C(CNC2=CC=C(C(OC)=O)C=C2)C=C(O)C=C1
InChi Code
InChI=1S/C15H15NO4/c1-20-15(19)10-2-4-12(5-3-10)16-9-11-8-13(17)6-7-14(11)18/h2-8,16-18H,9H2,1H3
InChi Key
QSFREBZMBNRGOK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    Product Description

    AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl (IC50s = 4.3, 1, and 7.1 µM, respectively, for human proteins).1 It also inhibits epidermal growth factor receptor (IC50 = 0.25 µM).1 As the constitutively-active 210 kDa Bcr-Abl fusion protein commonly occurs in chronic myelogenous leukemia (CML) cells, AG957 is commonly used to study Bcr-Abl signaling in the CML K562 cell line.2,3 AG957 is also used to study signaling through c-Abl.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Anafi, M., Gazit, A., Gilon, C., et al. Selective interactions of transforming and normal abl proteins with ATP, tyrosine-copolymer substrates, and tyrphostins. The Journal of Biological Chemisty 267(8), 4518-4523 (1992).

    2. Kaur, G., Gazit, A., Levitzki, A., et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anticancer Drugs 5(2), 213-222 (1994).

    3. Jamieson, L., Carpenter, L., Biden, T.J., et al. Protein kinase Cι activity is necessary for Bcr-Abl-mediated resistance to drug-induced apoptosis. The Journal of Biological Chemisty 274(7), 3927-3930 (1999).

    4. Fu, P., Usatyuk, P.V., Lele, A., et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. Am. J. Physiol. Regul. Integr. Comp. Physiol. 308, L1025-L1038 (2015).