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Erbstatin Analog

BML-EI146

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EGFR inhibitor

Erbstatin is a novel inhibitor of the EGF receptor-associated tyrosine kinase. It is an unstable compound and is completely inactivated in serum in 30 minutes. Methyl 2,5-dihydroxycinnamate is a stable erbstatin analog retaining activity after a 60 minute incubation. It inhibits EGF receptor-associated tyrosine kinase in vitro (IC₅₀=0.77 µM). Inhibition is competitive with substrate and noncompetitive with ATP.

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Product Details

Alternative Name	Methyl 2,5-dihydroxycinnamate
Appearance	Yellow solid.
CAS	63177-57-1
Couple Target	EGFR
Couple Type	Inhibitor
Formula	C₁₀H₁₀O₄
MW	194.2
MeltingPoint	169-172°C
Purity	≥98% (TLC)
Solubility	Soluble in ethanol (25mg/ml), methanol or DMSO (25mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at room temperature. Stock solutions are stable for up to 3 months at -20°C.
Handling	Protect from light and oxygen.
Long Term Storage	Ambient
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Induction of mouse thymocyte apoptosis by inhibitors of tyrosine kinases is associated with dephosphorylation of nuclear proteins: Y. Azuma, et al.; Cell. Immunol. 152, 271 (1993), Abstract
Inhibition of Abelson oncogene function by erbstatin analogues: M. Kawada, et al.; Drugs Exp. Clin. Res. 19, 235 (1993), Abstract
Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T3 cells: K. Umezawa, et al.; FEBS Lett. 314, 289 (1992), Abstract
Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors: K. Umezawa, et al.; FEBS Lett. 260, 198 (1990), Abstract
In situ inhibition of tyrosine protein kinase by erbstatin: M. Imoto, et al.; Biochem. Int. 15, 989 (1987), Abstract

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Erbstatin Analog

BML-EI146

Product Details

Handling & Storage

Datasheet, Manuals, SDS & CofA

Manuals And Inserts

Certificate of Analysis

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