AGN 195183 structure
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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 195183AGN 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 |
|---|---|
| Synonym | More Synonyms |
| 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. |
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| Related Catalog | |
| References |
| 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℃ |
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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
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Name: Percent inhibition of BrdU incorporation into SK-BR-3 cells
Source: ChEMBL
Target: SK-BR-3
External Id: CHEMBL804955
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|
Name: Percent transcriptional activation of RAR gamma compared to 1 mM ATRA; NA indicates <...
Source: ChEMBL
Target: Retinoic acid receptor gamma
External Id: CHEMBL681084
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|
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
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|
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
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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
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|
Name: Percent inhibition of BrdU incorporation into T-47D cells
Source: ChEMBL
Target: T47D
External Id: CHEMBL815483
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|
Name: Enzymatic assay of human HDAC6 with commercial peptide substrate
Source: ChEMBL
Target: Histone deacetylase 6
External Id: CHEMBL4808149
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| 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 |