AGN-195183 (IRX-5183) is a potent and selective agonist of RARα ( K d =3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ. In Vitro AGN-195183 (IRX-5183; Compound 4) inhibits the growth of breast cancer cell lines, and is inactive in an in vivo model of topical irritation. AGN-195183 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3. AGN-195183 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. AGN-195183 is currently in Phase I/IIA clinical trials in cancer patients. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50 value: 3 nM (Kd),200 nM (EC80, RAR Trans)
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AGN-195183
CAS number：367273-07-2 molecular formula：C22H22ClF2NO4
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | HY-16684 | 4-[(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalene-2-carbonyl)amino]-2,6-difluorobenzoic acid | RC87L028HU | SCHEMBL5531052 | VTP-5183 | Q27288046 | AGN 195183 | BDBM50120065 | DB05653 | 4-[(4-Chloro-3-hydroxy-5,5,8,8-tetramethyl | ||
| CAS number | 367273-07-2 | molecular formula | C22H22ClF2NO4 |
| molecular weight | 437.86 g/mol | Exact mass | ≥99% |
| PSA | 86.600 Ų | logp | 6.4 |
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