Erbstatin analog

Erbstatin analog

CAT N°: 10010238
Price:

From 20.00 17.00

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.{14867} 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.{15639} Erbstatin analog is a stable, potent inhibitor of EGFR kinase activity. It is four-times more stable than erbstatin in calf serum{15639} and inhibits EGFR tyrosine kinase in vitro similar to erbstatin with an IC50 value of 0.14 µg/ml.{15639} 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.{15638}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 3-(2,5-dihydroxyphenyl)-2-propenoic acid, methyl ester
  • Correlated keywords
    • analogs EGF EGFR inhibitors inhibits inhibition tyrosine kinase DNA synthesis cell cycle proliferation cancers
  • Product Overview:
    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.{14867} 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.{15639} Erbstatin analog is a stable, potent inhibitor of EGFR kinase activity. It is four-times more stable than erbstatin in calf serum{15639} and inhibits EGFR tyrosine kinase in vitro similar to erbstatin with an IC50 value of 0.14 µg/ml.{15639} 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.{15638}

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