133550-35-3
Chemical Structure
AG-494
Synonym(s): Tyrphostin AG 494
- CAS No.: 133550-35-3
- Formula:C16H12N2O3
- Molecular Weight:280.28
IUPAC Name: (E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide
InChIKey: HKHOVJYOELRGMV-XYOKQWHBSA-N
SMILES: O=C(NC1=CC=CC=C1)/C(C#N)=C/C2=CC=C(O)C(O)=C2
Biological Activity: AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis[1][2][3].
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AG-494 | 98.69% | AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis. | ||||||||||||||||||||
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- [1]. Gazit A, et al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991;34(6):1896-1907. [Content Brief]
- [2]. Osherov N, et al. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997;410(2-3):187-190. [Content Brief]
- [3]. Osherov N, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem. 1993 May 25;268(15):11134-42. [Content Brief]
Keywords