RG-13022

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC₅₀ value of 1 μM in HT-22 cells.

(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells[1][2].

ChEBI: 3-(3,4-dimethoxyphenyl)-2-(3-pyridinyl)-2-propenenitrile is a dimethoxybenzene.

[1] Reddy KB, et al. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res. 1992 Jul 1;52(13):3636-41. PMID:1617636
[2] McLeod HL, et al. In vivo pharmacology and anti-tumour evaluation of the tyrphostin tyrosine kinase inhibitor RG13022. Br J Cancer. 1996 Dec;74(11):1714-8. DOI:10.1038/bjc.1996.620