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RG13022 is a non-phenolic tyrphostin-class tyrosine kinase inhibitor. RG13022 inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM. RG13022 inhibits colony formation and DNA synthesis by HER 14 cells, which were stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s are 1 and 3 μM for HER 14 colony formation and DNA synthesis, respectively. RG-13022 also totally blocks estrogen-stimulated phosphorylation of the EGF receptor, as well as estrogen-induced cell proliferation, suggesting that functioning TK pathways are required for estrogen action.
In vivo, RG13022 suppresses tumor growth in nude mice. RG13022 also increases the life span of these tumor-bearing nude mice.
| Molecular Weight | 266.29 |
| Formula | C16H14N2O2 |
| CAS Number | 136831-48-6 |
| Solubility (25°C) | Soluble in DMSO Soluble in ethanol |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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