Androgen receptor antagonist 1
Modify Date: 2024-01-03 09:12:36
Androgen receptor antagonist 1 structure
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Common Name | Androgen receptor antagonist 1 | ||
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| CAS Number | 1338812-36-4 | Molecular Weight | 416.90 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H25ClN4O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Androgen receptor antagonist 1Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2]. |
| Name | Androgen receptor antagonist 1 |
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| Description | Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2]. |
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| Related Catalog | |
| Target |
IC50: 59 nM (androgen receptor)[1] |
| In Vitro | Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 cells[1]. Cell Proliferation Assay[1] Cell Line: Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145) Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM Incubation Time: 7 days Result: Antiproliferative effects of in LNCAP and LNAR cells. |
| In Vivo | Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model[1]. Animal Model: Male athymic nude mice with LNCaP xenograft model of CRPC[1] Dosage: 100 mg/kg Administration: Orally once a day for 5 weeks Result: Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated. |
| References |
| Molecular Formula | C21H25ClN4O3 |
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| Molecular Weight | 416.90 |
| InChIKey | HJJNHDLYWZTKGQ-UHFFFAOYSA-N |
| SMILES | CC1(C)C(NC(=O)c2cnn(CCO)c2)C(C)(C)C1Oc1ccc(C#N)c(Cl)c1 |
| Hazard Codes | Xi |
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