产品
编 号：F624510
分子式：C21H25ClN4O3
分子量：416.9
分子式：C21H25ClN4O3
分子量：416.9
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 1338812-36-4
产品详情
生物活性：
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. 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.
体内研究：
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.Animal Model:Male athymic nude mice with LNCaP xenograft model of CRPC
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.
体外研究：
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.
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. 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.
体内研究：
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.Animal Model:Male athymic nude mice with LNCaP xenograft model of CRPC
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.
体外研究：
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.
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