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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.
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RUO – Research Use Only |
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