AGN 195183

Names

[ Name ]:
AGN 195183

[Synonym ]:
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-

Biological Activity

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
500.9±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₂H₂₂ClF₂NO₄

[ Molecular Weight ]:
437.864

[ Flash Point ]:
256.7±30.1 °C

[ Exact Mass ]:
437.120544

[ LogP ]:
9.02

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.596

[ Storage condition ]:
2-8℃

Related Compounds

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