113299-40-4
113299-40-4 structure
- Name: (R)-Bicalutamide
- Chemical Name: (R)-Bicalutamide
- CAS Number: 113299-40-4
- Molecular Formula: C18H14F4N2O4S
- Molecular Weight: 430.373
- Catalog: Signaling Pathways Others Androgen Receptor
- Create Date: 2018-09-16 11:44:30
- Modify Date: 2024-01-02 10:09:02
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(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer[1][2].
| Name | (R)-Bicalutamide |
|---|---|
| Synonyms |
(2R)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
Propanamide, N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-, (2R)- (1E,2R)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanimidic acid R-bicalutamide Bicalutamide Propanimidic acid, N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-, (1E,2R)- R-Bicalutimide MFCD00870866 Bicalutamide Impurity 2 |
| Description | (R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer[1][2]. |
|---|---|
| Related Catalog | |
| Target |
AR[1] |
| In Vitro | Bicalutamide (HY-14249) is available as a racemic mixture. The R isomer (R-bicalutamide) has an ≈30-fold higher binding affinity to the AR than the S isomer[1]. (R)-bicalutamide (0.02-20 μM) reduces naïve LNCaP cells survival in a dose-dependent[2]. Cell Proliferation Assay[2] Cell Line: LNCaP cells, LNCaP-Rbic cells Concentration: 0.02 μM, 0.2 μM, 2 μM, 20 μM Incubation Time: 144 hours Result: Reduced naïve LNCaP cells survival in a dose-dependent, with an IC 50 value of about 7μM; exerted a poor antiproliferative effect on LNCaP-Rbic. |
| In Vivo | (R)-Bicalutamide (10 mg/kg; i.g.; daily; for 4 days) has antitumor efficacy in VCaP xenografts mice[3]. Animal Model: CD1 male nude (nu/nu) mice, with VCaP xenografts[3] Dosage: 10 mg/kg Administration: Orally gavage, daily, for 4 consecutive weeks Result: Suppressed tumor growth. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 650.3±55.0 °C at 760 mmHg |
| Melting Point | 178-181ºC |
| Molecular Formula | C18H14F4N2O4S |
| Molecular Weight | 430.373 |
| Flash Point | 347.1±31.5 °C |
| Exact Mass | 430.061035 |
| PSA | 115.64000 |
| LogP | 4.94 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Index of Refraction | 1.578 |
| Storage condition | -20?C Freezer |