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HOME> Products> Natural and Chemical compound> Erbstatin
HOME> Products> Natural and Chemical compound> Enzyme inhibitor> Erbstatin

Tyrosine kinase inhibitor Erbstatin

Date：April 14 2022Web Page No：95021

Institute of Microbial Chemistry

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.

Specification
Mechanism
Application Notes
References

Specification

CAS#	100827-28-9
Molecular Formula	C₉H₉NO₃
Molecular Weight	179.175
Source	Streptomyces sp. MH435-hF3
Purity	>98% (HPLC)
Solubility	Soluble in MeOH, DMSO and Acetone Insoluble in Hexane and H₂O

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Mechanism

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

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

[Date : June 03 2024 00:06]

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

Contact

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

[Date : June 03 2024 00:06]

Erbstatin,Tyrosine Kinase Inhibitor (TKI)

DatasheetThis may not be the latest data sheet.

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

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

Contact

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