AGN 195183 (Synonyms: IRX-5183; VTP-195183; NRX-195183) |
| カタログ番号GC35265 |
AGN 195183 (IRX-5183) は、AGN 193836 に比べて結合選択性が向上した RARα (Kd = 3 nM) の強力かつ選択的なアゴニストです。
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Cas No.: 367273-07-2
Sample solution is provided at 25 µL, 10mM.
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AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.)Target: RARα agonistCompound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation.Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients.
[1]. Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.
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