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Tyrosine kinase inhibitor Erbstatin

Date:April 14 2022Web Page No:95021

Erbstatin is a natural product derived from actinomycetes. It inhibits receptor-type tyrosine kinases such as EGFR tyrosine kinase without inhibiting cAMP-dependent protein kinase or protein kinase C.

Erbstatin

Specification

CAS#100827-28-9
Molecular FormulaC9H9NO3
Molecular Weight179.175
SourceStreptomyces sp. MH435-hF3
Purity>98% (HPLC)
SolubilitySoluble in MeOH, DMSO and Acetone
Insoluble in Hexane and H2O

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Mechanism

Mechanism of tyrosine kinase inhibitory activity by Erbstatin

EGF receptor bound to EGF activates its own tyrosine kinase (TK) and autophosphorylates. Grb2-Sos attaches to this phosphotyrosine and stimulates Ras. The stimulated Ras activates Ras signaling pathway, leading to gene expression involved in proliferation and malignant transformation of cancer. Erbstatin inhibits TK of the EGF receptor, thereby blocking activation of the Ras-signaling-pathway and inhibiting malignant transformation of cancer 1).

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Application Notes

  • Inhibits EGF receptor-autophosphorylation but not inhibit cyclic AMP dependent protein kinase (IC50: 0.55 ug/ml) 1)
  • Inhibits the growth of human epidemoid carcinoma (A-431 cells) (IC50: 3.6 ug/ml) 1)
  • Inhibits mouse IMC carcinoma cells (IC50: 3.01 ug/ml) 1)
  • Has weak antibacterial activity in mouse intraperitoneal administration (LD50: >200 mg/kg) 1)
  • Shows antineoplastic activity against L-1210 mouse leukemia when it is injected together with foroxymithine which stabilizes erbstatin in serum 4)

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References

  1. Umezawa, H., et al., J. Antibiot., 39 (1), 170~173 (1986). [PMID:3005217]
  2. Nakamura, H., et al., J. Antibiot., 39 (2), 314~315 (1986). [PMID:3007417]
  3. Imoto, M., et al., J. Antibiot., 40 (10), 1471~1743 (1987). [PMID:3680017]
  4. Imoto, M., et al., Jpn. J. Cancer Res., 78 (4), 329~332 (1987). [PMID:3108212]

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[Date : June 20 2024 00:07]

Detail Product Name Product Code Supplier Size Price
Erbstatin,Tyrosine Kinase Inhibitor (TKI)
DatasheetThis may not be the latest data sheet.
14697 IMCInstitute of Microbial Chemistry 1 mg $500

Description
Storage -20°C CAS 100827-28-9
Link

Bioactive Compounds

[Date : June 20 2024 00:07]

Erbstatin,Tyrosine Kinase Inhibitor (TKI)


  • Product Code: 14697
  • Supplier: IMC
  • Size: 1mg
  • Price: $500

Description
Storage -20°C CAS 100827-28-9
Link

Bioactive Compounds


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