Erbstatin (Tyrosine Kinase Inhibitor (TKI))
Erbstatin <Tyrosine Kinase Inhibitor (TKI)>
Cat No: FNK-14697
Size: 1 mg
Specifications
Code No. : 14697
CAS# : 100827-28-9
Molecular Formula : C9H9NO3
Molecular Weight : 179.175
Source : Streptomyces sp. MH435-hF3
Supplied as : Powder Purity : >90% (HPLC)
Long Term Storage : at -20 °C
Solubility : Soluble in MeOH, DMSO, Acetone Insoluble in Hexane, H2O
Application Notes
Erbstatin was isolated from the culture filtrate of Streptomyces sp. MH435-hF3 as an inhibitor of epidermal growth factor (EGF) receptor associated tyrosine kinase. 1-3) It inhibits EGF receptorautophosphorylation with IC50 of 0.55 μg/ml in vitro, but it does not inhibit cyclic AMP dependent protein kinase. 1) Erbstatin inhibits the growth of human epidemoid carcinoma (A-431 cells) (IC50 3.6 μg/ml) and IMC-carcinoma cells (IC50 3.01 μg/ml). 1) It has weak antibacterial activity and low toxicity (LD50 >200 mg/kg mice ip). 1) Erbstatin shows antineoplastic activity against L-1210 mouse leukemia when it is injected together with foroxymithine which stabilizes erbstatin in serum. 4)
References
1) Studies on a new epidermal growth factor-receptor kinase inhibitor, erbstatin, produced by MH435-hF3. Umezawa H, et al. J Antibiot. 1986 39(1) 170-173. 2) The structure of an epidermal growth factor-receptor kinase inhibitor, erbstatin. Nakamura H, et al. J Antibiot. 1986 39(2) 314- 315. 3) Kinetic studies of tyrosine kinase inhibition by erbstatin. Imoto M, et al. J Antibiot. 1987 40(10) 1471-1473. 4) Antitumor activity of erbstatin, a tyrosine protein kinase inhibitor. Imoto M, et al. Jpn J. Cancer Res. 1987 78(4) 329-332.
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