367273-07-2

367273-07-2 structure

Name: AGN 195183
Chemical Name: AGN 195183
CAS Number: 367273-07-2
Molecular Formula: C₂₂H₂₂ClF₂NO₄
Molecular Weight: 437.864
Catalog: Signaling Pathways Metabolic Enzyme/Protease RAR/RXR
Create Date: 2018-05-24 23:22:35
Modify Date: 2024-01-08 17:12:03
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.

Name	AGN 195183
Synonyms	4-{[(4-Chloro-3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-2-naphthalenyl)carbonyl]amino}-2,6-difluorobenzoic acid RC87L028HU 4-{[(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbonyl]amino}-2,6-difluorobenzoic acid IRX-5183 Benzoic acid, 4-[[(4-chloro-5,6,7,8-tetrahydro-3-hydroxy-5,5,8,8-tetramethyl-2-naphthalenyl)carbonyl]amino]-2,6-difluoro-

Description	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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR Research Areas >> Cancer
References	[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.