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编 号：F756605
分子式：C29H36N4O
分子量：456.62
分子式：C29H36N4O
分子量：456.62
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CAS No: 2883447-45-6
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生物活性：
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM.
体内研究：
AR antagonist 4 (Compound 67-b) (20 mg/kg; p.o.; daily for 10 days) inhibits the growth of androgen-sensitive organs (ASOs) under the stimulation of testosterone propionate (TP) in rats.AR antagonist 4 (30 mg/kg; p.o.; daily for 4 weeks) shows antitumor activity in an Enzalutamide (HY-70002)-resistant c4-2b?ENZ xenograft model in mice.Animal Model:Castrated male Sprague?Dawley rats
Dosage:20 mg/kg
Administration:Oral administration, daily for 10 days
Result:Resulted in statistically significant weight reductions in seminal vesicles (62%, p < 0.01) and ventral prostate (66%, p <0.01) versus the testosterone propionate control.
Animal Model:SPF grade male Babl/c nude male mice, enzalutamide-resistant c4-2b?ENZ xenograft model
Dosage:30 mg/kg
Administration:Oral administration, daily for 4 weeks
Result:Exhibited a remarkable tumor regression with ΔT/ΔC% = ?14% after 4 weeks of treatment.
Animal Model:Male Sprague?Dawley rats
Dosage:10 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:PK Parameters for AR antagonist 4 (Compound 67-b) in Male SD RatsaCompoundT1/2 (h) Tmax (h) Cmax (ng/mL)AUC0-t (ng?h/mL)
AR antagonist 42.802.17267024 800
aCompounds were PO-dosed at 10 mg/kg in a solution of 5% DMSO + 30% PEG400 + 65% water (0.5% MC) in male SD rats. Abbreviations: Cmax, maximum drug concentration; AUC0-t, area under the curve between 0 and t h; T1/2, terminal half-life; Tmax, the time taken to reach Cmax.Values are expressed as the mean, n = 3.
体外研究：
AR antagonist 4 (Compound 67-b) (0-10 μM; 6 days) inhibits LNCaP and 22RV1 cells proliferation.AR antagonist 4 inhibits CYP17A1 with an IC50 of 2.59 μM.AR antagonist 4 shows antagonistic activities with IC50s of 490.2, 208.8 and 268.2 nM against AR(W741L), AR(T877A) and AR (F876L), respectively.
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM.
体内研究：
AR antagonist 4 (Compound 67-b) (20 mg/kg; p.o.; daily for 10 days) inhibits the growth of androgen-sensitive organs (ASOs) under the stimulation of testosterone propionate (TP) in rats.AR antagonist 4 (30 mg/kg; p.o.; daily for 4 weeks) shows antitumor activity in an Enzalutamide (HY-70002)-resistant c4-2b?ENZ xenograft model in mice.Animal Model:Castrated male Sprague?Dawley rats
Dosage:20 mg/kg
Administration:Oral administration, daily for 10 days
Result:Resulted in statistically significant weight reductions in seminal vesicles (62%, p < 0.01) and ventral prostate (66%, p <0.01) versus the testosterone propionate control.
Animal Model:SPF grade male Babl/c nude male mice, enzalutamide-resistant c4-2b?ENZ xenograft model
Dosage:30 mg/kg
Administration:Oral administration, daily for 4 weeks
Result:Exhibited a remarkable tumor regression with ΔT/ΔC% = ?14% after 4 weeks of treatment.
Animal Model:Male Sprague?Dawley rats
Dosage:10 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:PK Parameters for AR antagonist 4 (Compound 67-b) in Male SD RatsaCompoundT1/2 (h) Tmax (h) Cmax (ng/mL)AUC0-t (ng?h/mL)
AR antagonist 42.802.17267024 800
aCompounds were PO-dosed at 10 mg/kg in a solution of 5% DMSO + 30% PEG400 + 65% water (0.5% MC) in male SD rats. Abbreviations: Cmax, maximum drug concentration; AUC0-t, area under the curve between 0 and t h; T1/2, terminal half-life; Tmax, the time taken to reach Cmax.Values are expressed as the mean, n = 3.
体外研究：
AR antagonist 4 (Compound 67-b) (0-10 μM; 6 days) inhibits LNCaP and 22RV1 cells proliferation.AR antagonist 4 inhibits CYP17A1 with an IC50 of 2.59 μM.AR antagonist 4 shows antagonistic activities with IC50s of 490.2, 208.8 and 268.2 nM against AR(W741L), AR(T877A) and AR (F876L), respectively.
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