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AG-494

EGFR inhibitor
 
BML-EI228-0010 10 mg 74.00 USD
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Replaces Prod. #: ALX-270-143

AG-494 is a member of the tyrphostin family of tyrosine kinase inhibitors and is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 µM) and EGF-dependent cell growth (IC50=6 µM). It selectively inhibits HER1 (EGF receptor) vs. HER1-2 receptor autophosphorylation (HER1: IC50=1.1 µM; HER1-2: IC50=45 µM). HER1-2 is a chimeric receptor consisting of the external HER1 domain fused to an internal HER2 domain. Blocks CDK2 activation and causescells to arrest at late G1 and during S phase.

Product Specification

Formula:C16H12N2O3
 
MW:280.3
 
CAS:133550-35-3
 
Purity:≥98% (TLC)
 
Appearance:Yellow solid.
 
Solubility:Soluble in DMSO (25mg/ml) or 100% ethanol (25mg/ml).
 
Shipping:Ambient
 
Long Term Storage:Ambient
 
Use/Stability:Product is subject to oxidation.
 
Handling:Store tightly sealed in the dark. Protect from light. Make solutions fresh daily.
 
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Product Literature References

Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase: N. Kleinberger-Doron, et al.; Exp. Cell Res. 241, 340 (1998), Abstract;
Tyrphostin AG 494 blocks Cdk2 activation: N. Osherov & A. Levitzki; FEBS Lett. 410, 187 (1997), Abstract;
Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins: N. Osherov, et al.; J. Biol. Chem. 268, 11134 (1993), Abstract;
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases: A. Gazit, et al.; J. Med. Chem. 34, 1896 (1991), Abstract;

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