AGN 195183是RARα选择性激动剂，Kd为3 nM，相对于AGN 193836有更好的结合选择性，对RARβ/γ无活性。
CAS：367273-07-2
分子式：C22H22ClF2NO4
分子量：437.86
纯度：98%
存储：Store at -20°C

Background:

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.

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