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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Erbstatin Analog

Cayman Chemical Item Number 10010238

Methyl 2,5-dihydoxycinnamate (CAS 63177-57-1)

Erbstatin Analog (CAS 63177-57-1)

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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.1 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.2 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.2 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.3

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 Lett 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 Lett 314(3) 289-292 (1992).

Synonyms
  • Methyl 2,5-dihydoxycinnamate
Formal Name 3-​(2,​5-​dihydroxyphenyl)-​2-​propenoic acid,​ methyl ester
CAS Number 63177-57-1
Molecular Formula C10H10O4
Formula Weight 194.2
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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COC(=O)​\C=C/c1cc(O)​ccc1O

Background Reading

Umezawa, K., Hori, T., Tajima, H., et al. Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors. FEBS Lett 260(2) 198-200 (1990).

Umezawa, K., Sugata, D., Yamashita, K., et al. Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T3 cells. FEBS Lett 314(3) 289-292 (1992).

Sausville, E.A., Elsayed, Y., Monga, M., et al. Signal transduction-directed cancer treatments. Annu Rev Pharmacol Toxicol 43 199-231 (2003).

Erbstatin Analog is available in the following screening library:

Size Price Quantity Subtotal
1 mg $9.00 $0.00
5 mg $41.00 $0.00
10 mg $72.00 $0.00
50 mg $315.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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