AGN 195183

Modify Date: 2026-07-03 12:01:39

AGN 195183 Structure
AGN 195183 structure
Common Name AGN 195183
CAS Number 367273-07-2 Molecular Weight 437.864
Density 1.4±0.1 g/cm3 Boiling Point 500.9±50.0 °C at 760 mmHg
Molecular Formula C22H22ClF2NO4 Melting Point N/A
MSDS N/A Flash Point 256.7±30.1 °C

 Use of AGN 195183


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.

 Names

Name AGN 195183
Synonym More Synonyms

 AGN 195183 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
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.

 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
InChIKey PNAWUIKCVQSLFG-UHFFFAOYSA-N
SMILES CC1(C)CCC(C)(C)c2c1cc(C(=O)Nc1cc(F)c(C(=O)O)c(F)c1)c(O)c2Cl
Storage condition 2-8℃

 AGN 195183Bioassay

View more

Name: Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER...
Source: ChEMBL
Target: Severe acute respiratory syndrome coronavirus 2
External Id: CHEMBL4513082
Name: Percent inhibition of BrdU incorporation into SK-BR-3 cells
Source: ChEMBL
Target: SK-BR-3
External Id: CHEMBL804955
Name: Percent transcriptional activation of RAR gamma compared to 1 mM ATRA; NA indicates <...
Source: ChEMBL
Target: Retinoic acid receptor gamma
External Id: CHEMBL681084
Name: Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac...
Source: ChEMBL
Target: Severe acute respiratory syndrome coronavirus 2
External Id: CHEMBL4303805
Name: SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f...
Source: ChEMBL
Target: Replicase polyprotein 1ab
External Id: CHEMBL4495582
Name: Cytotoxicity against African green monkey COS7 cells assessed as cell death after 2 d...
Source: ChEMBL
Target: COS-7
External Id: CHEMBL4187057
Name: Transactivation of mouse Gal4-fused RARalpha-LBD expressed in COS-7 cells after 1 day...
Source: ChEMBL
Target: Retinoic acid receptor alpha
External Id: CHEMBL4187003
Name: Transactivation of mouse Gal4-fused RARbeta-LBD expressed in COS-7 cells after 1 day ...
Source: ChEMBL
Target: Retinoic acid receptor beta
External Id: CHEMBL4187005
Name: Percent inhibition of BrdU incorporation into T-47D cells
Source: ChEMBL
Target: T47D
External Id: CHEMBL815483
Name: Enzymatic assay of human HDAC6 with commercial peptide substrate
Source: ChEMBL
Target: Histone deacetylase 6
External Id: CHEMBL4808149
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 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
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