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