140674-76-6
140674-76-6 structure
- Name: Tyrphostin AG 957
- Chemical Name: methyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate
- CAS Number: 140674-76-6
- Molecular Formula: C15H15NO4
- Molecular Weight: 273.28400
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Bcr-Abl
- Create Date: 2017-04-05 08:24:38
- Modify Date: 2024-01-10 11:49:30
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AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].
| Name | methyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate |
|---|---|
| Synonyms |
N-(2,5-dihydroxylbenzyl)-4-methoxycarbonyl aniline
methyl 4-(N-2,5-dihydroxybenzylamino)benzoate AG 957 4-Amino-N-(2,5-dihydroxybenzyl)methyl benzoate Tyrphostin AG 957 Benzoic acid,4-[[(2,5-dihydroxyphenyl)methyl]amino]-,methyl ester methyl 4-[(2,5-dihydroxybenzyl)amino]benzoate |
| Description | AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3]. |
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| Related Catalog | |
| In Vitro | AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1].Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2]. AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2]. AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2]. Cell Proliferation Assay[2] Cell Line: CML and CFC Concentration: 0, 0.1, 1, 10, 100 μM Incubation Time: Pretreatment for 1 hour Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957. Western Blot Analysis[2] Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4) Concentration: 25 μM Incubation Time: 24 hours Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells. Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells. |
| 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 |
| Molecular Formula | C15H15NO4 |
|---|---|
| Molecular Weight | 273.28400 |
| Exact Mass | 273.10000 |
| PSA | 78.79000 |
| LogP | 2.56950 |
| Storage condition | -20°C |
| Hazard Codes | Xi |
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