Erbstatin analog

Overactivity of the epidermal growth factor (EGF) receptor-associated tyrosine kinase has been associated with a number of cancers and thus tyrosine kinase inhibitors could be potential therapeutic agents to prevent malignant growth. Erbstatin is a potent, small-molecule inhibitor of EGF receptor-associated tyrosine kinase. However, it is highly unstable, inactivating completely within 30 minutes in calf serum. Erbstatin analog is a stable, potent inhibitor of EGFR kinase activity. It is four-times more stable than erbstatin in calf serum and inhibits EGFR tyrosine kinase in vitro similar to erbstatin with an IC50 value of 0.14 µg/ml. Erbstatin analog inhibits EGF-stimulated growth in EGFR-overexpressing NIH3T3 cells with an IC50 value of 0.5 µg/ml and efficiently delays the onset of EGF-induced DNA synthesis.Formal Name: 3-(2,5-dihydroxyphenyl)-2-propenoic acid, methyl ester. CAS Number: 63177-57-1. Synonyms: Methyl 2,5-dihydoxycinnamate. Molecular Formula: C10H10O4. Formula Weight: 194.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Ethanol: 10 mg/ml. lambdamax: 250, 280, 362 nm. SMILES: COC(=O)\C=C/c1cc(O)ccc1O. InChi Code: InChI=1S/C10H10O4/c1-14-10(13)5-2-7-6-8(11)3-4-9(7)12/h2-6,11-12H,1H3/b5-2+. InChi Key: BQCNSTFWSKOWMA-GORDUTHDSA-N.