Product Overview
AGN-195183 | T14144 | TargetMol Chemicals
CAS: 367273-07-2
Smiles: CC1(C)CCC(C)(C)c2c(Cl)c(O)c(cc12)C(=O)Nc1cc(F)c(C(O)=O)c(F)c1
Formula: C22H22ClF2NO4
Pathway: Others
Target: Others
Receptor: N/A
Bioactivity: 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 agonist Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients. Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, however it does not cause the topical irritation induced by the RARa-selective retinoid, Am-580.
Molecular Weight: 437, 87
