AG 957 Chemical Properties

Boiling point:

504.2±45.0 °C(Predicted)

Density 

1.337±0.06 g/cm3(Predicted)

storage temp. 

−20°C

solubility 

DMSO: soluble

form 

crystalline solid

pka

10.30±0.43(Predicted)

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

AG 957 Usage And Synthesis

Description

Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases. AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185^Bcr-Abl, p210^Bcr-Abl), as well as normal c-Abl (IC₅₀s = 4.3, 1, and 7.1 μM, respectively, for human proteins). It also inhibits epidermal growth factor receptor (IC₅₀ = 0.25 μM). 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. AG957 is also used to study signaling through c-Abl.

Uses

Tyrphostin AG 957 is a potent tyrosine kinase inhibitor. Also, it causes metabolic alterations in K562 cells. It is a COVID19-related research product.

Definition

ChEBI: 4-[(2,5-dihydroxyphenyl)methylamino]benzoic acid methyl ester is an aromatic amine.

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. j biol chem. 1992 mar 5;267(7):4518-23.
[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. 1994 apr;5(2):213-22.
[3]. jamieson l, carpenter l, biden tj, et al. protein kinase ciota activity is necessary for bcr-abl-mediated resistance to drug-induced apoptosis. j biol chem. 1999 feb 12;274(7):3927-30.
[4]. fu p, usatyuk pv, lele a, et al. c-abl mediated tyrosine phosphorylation of paxillin regulates lps-induced endothelial dysfunction and lung injury. am j physiol lung cell mol physiol. 2015 may 15;308(10):l1025-38.

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