ChemicalBook > CAS DataBase List > AG 957

AG 957

Product Name
AG 957
CAS No.
140674-76-6
Chemical Name
AG 957
Synonyms
AG 957;NSC 654705;TYRPHOSTIN 957;TYRPHOSTIN AG 957;LAVENDUSTIN C ANALOG;AG957, 10 mM in DMSO;Methyl 4-((2,5-dihydroxybenzyl)amino)benzoate;4-AMINO-N-(2,5-DIHYDROXYBENZYL)METHYL BENZOATE;Tyrphostin AG 957, p210 tyrosine kinase inhibitor;METHYL-4-[N-(2',5'-DIHYDROXYBENZYL)AMINO]BENZOATE
CBNumber
CB6100142
Molecular Formula
C15H15NO4
Formula Weight
273.28
MOL File
Mol file
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AG 957 Property

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)
color 
Off-white to light brown
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Safety

Safety Statements 
22-24/25
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17259
Product name
AG957
Purity
≥95%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
17259
Product name
AG957
Purity
≥95%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
17259
Product name
AG957
Purity
≥95%
Packaging
10mg
Price
$213
Updated
2024/03/01
TRC
Product number
T947970
Product name
TyrphostinAG957
Packaging
1mg
Price
$40
Updated
2021/12/16
ApexBio Technology
Product number
C5826
Product name
AG957
Packaging
5mg
Price
$124
Updated
2021/12/16
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AG 957 Chemical Properties,Usage,Production

Description

Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases. 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). 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.

in vivo

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

Animal Model:C57BL/6J mice[4]
Dosage:10 mg/kg
Administration:Intratracheally 1 h before intratracheal LPS challenge
Result:LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.

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.

AG 957 Preparation Products And Raw materials

Raw materials

Preparation Products

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AG 957 Suppliers

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140674-76-6, AG 957Related Search:


  • METHYL-4-[N-(2',5'-DIHYDROXYBENZYL)AMINO]BENZOATE
  • LAVENDUSTIN C ANALOG
  • 4-AMINO-N-(2,5-DIHYDROXYBENZYL)METHYL BENZOATE
  • AG 957
  • TYRPHOSTIN AG 957
  • TYRPHOSTIN 957
  • NSC 654705
  • Lavendustin C Analog, Methyl-4-[N-(2μ,5μ-dihydroxybenzyl)amino]benzoate
  • Benzoic acid, 4-[[(2,5-dihydroxyphenyl)methyl]amino]-, methyl ester
  • paxillin,NSC654705,c-Abl,Bcr-Abl,lipopolysaccharide,Tyrphostin AG-957,integrins,leukemia,tyrosine,Tyrphostin AG 957,hematopoiesis,AG-957,NSC-654705,AG 957,NSC 654705,AG957,Tyrphostin AG957,kinase,BCR/ABL,inhibit,cytoskeleton,Inhibitor,Chronic,myelogenous
  • Tyrphostin AG 957, p210 tyrosine kinase inhibitor
  • AG957, 10 mM in DMSO
  • Methyl 4-((2,5-dihydroxybenzyl)amino)benzoate
  • 140674-76-6
  • BioChemical
  • Cell Signaling and Neuroscience
  • Cell Biology
  • Kinase/Phosphatase Biology
  • Receptor Tyrosine Kinase Inhibitors
  • Tyrosine Kinase (TK)