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Erbstatin analog (CAS 63177-57-1) LS-H37

EGFR inhibitor
LS-H37-1 / 1 mg / $165
LS-H37-5 / 5 mg / $185
LS-H37-10 / 10 mg / $215
LS-H37-50 / 50 mg / $385
USA Shipment Only
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Description: 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 ug/ml. Erbstatin analog inhibits EGF-stimulated growth in EGFR-overexpressing NIH3T3 cells with an IC50 value of 0.5 ug/ml and efficiently delays the onset of EGF-induced DNA synthesis. H37_ChemicalStructureImage.png
3-(2,5-dihydroxyphenyl)-2-propenoic acid, methyl ester
Methyl 2,5-dihydoxycinnamate
biochemical, chemical, inhibitor
A crystalline solid
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: EGFR related products

Usage Information

Erbstatin analog is supplied as a crystalline solid. A stock solution may be made by dissolving the erbstatin analog in the solvent of choice. Erbstatin analog is soluble in the organic solvent ethanol, which should be purged with an inert gas. The solubility of erbstatin analog in ethanol is approximately 10 mg/ml. Erbstatin analog is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

  1. Sausville, E.A., Elsayed, Y., Monga, M., et al. Signal transduction-directed cancer treatments. Annu. Rev. Pharmacol. Toxicol. 43, 199-231 (2003).
  2. Umezawa, K., Hori, T., Tajima, H., et al. Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors. FEBS 260(2), 198-200 (1990).
  3. Umezawa, K., Sugata, D., Yamashita, K., et al. Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T3 cells. FEBS 314(3), 289-292 (1992).

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