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Tyrphostin AG 1024, 1 mg  

Tyrphostin AG 1024, 1 mg

2-[(3-bromo-4-hydroxy-5-tert-butyl-phenyl)methylidene]propanedinitrile

Synonyms: Tyrphostin AG1024, AG-1024
inhibitor of IGF-1R and IR

More details

PKI-AG1024-001

Availability: within 3 days

140,00 €

Background: Tyrphostin AG 1024 is a Insulin like growth factor receptor kinase (IGF-1R) and Insulin receptor kinase (IR) inhibitor with a IC50 value of 0.4 µM (IGF-1R) and 0.1µM (IR). In a human breast cancer cell line (MCF-7) the exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in a time-dependent manner. The IGF-1 inhibitor was also able to markedly increase the response of tumour cells to ionizing radiation. Tyrphostin AG1024 was shown to downregulate expression of BCR-ABL and P-Akt and was also effective against cells resistant to the BCR-ABL inhibitor STI571.

Chemicla formula: C14H13BrN2O
Molecular Weight: 305.2 g/mol
Purity: >98%
Appearance: yellow solid
Solubility: in DMSO
CAS Nr. 65678-07-1

Product specific literature references:

Wen B, Deutsch E, Marangoni E, Frascona V, Maggiorella L, Abdulkarim B, Chavaudra N, Bourhis J (2001) " Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells" Br. J. Cancer 85(12):2017-21.von Willebrand M, Zacksenhaus E, Cheng E, Glazer P, Halaban R. (2003) " The tyrphostin AG1024 accelerates the degradation of phosphorylated forms of retinoblastoma protein (pRb) and restores pRb tumor suppressive function in melanoma cells." Cancer Res. 63(6):1420-9.

Parrizas M, Gazit A, Levitzki A, Wertheimer E, LeRoith D (1997) " Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins" Endocrinology 138 (4):1427-33.

Deutsch E, Maggiorella L, Wen B, Bonnet ML, Khanfir K, Frascogna V, Turhan AG, Bourhis J. (2004) "Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation" Br. J. Cancer 91 (9): 1735-41.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.