2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. AR antagonist 4

AR antagonist 4 (Compound 67-b) 是一种具有口服活性的雄激素受体 (AR) 拮抗剂，对野生型 AR 的 IC50 为 246.6 nM，也是 AR 的降解剂，DC50 为 2.84 μM。

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AR antagonist 4 Chemical Structure

AR antagonist 4 Chemical Structure

CAS No. : 2883447-45-6

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AR antagonist 4 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 208.8 nM (AR(T877A)), 246.6 nM (wt-AR), 268.2 nM (AR (F876L)), 490.2 nM (AR(W741L))[1]
DC50: 2.84 μM (AR)[1]
体外研究
(In Vitro)

AR antagonist 4 (Compound 67-b) (0-10 μM; 6 days) inhibits LNCaP and 22RV1 cells proliferation[1].
AR antagonist 4 inhibits CYP17A1 with an IC50 of 2.59 μM[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AR antagonist 4 相关抗体:

Cell Proliferation Assay[1]

Cell Line: LNCaP and 22RV1 cells
Concentration: 0-10 μM
Incubation Time: 6 days
Result: Showed antiproliferative activity with IC50s of 246.6 nM and 590 nM against LNCaP and 22RV1 cells, respectively.

Western Blot Analysis[1]

Cell Line: LNCaP and 22RV1 cells
Concentration: 0, 1, 5, 10 and 20 μM
Incubation Time: 0, 2, 4, 8, 16 and 24 h
Result: Degraded androgen receptor in a dose- and time- dependent manner.
体内研究
(In Vivo)

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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Castrated male Sprague−Dawley rats[1]
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[1]
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[1]
Dosage: 10 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: PK Parameters for AR antagonist 4 (Compound 67-b) in Male SD Ratsa[1]
Compound T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng•h/mL)
AR antagonist 4 2.80 2.17 2670 24 800
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.
分子量

456.62

Formula

C29H36N4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AR antagonist 4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

AR antagonist 42883447-45-6AR antagonist4AR antagonist-4Androgen ReceptorLNCaP22RV1antitumorAR(W741L)AR(T877A)AR (F876L)mCRPCcastration-resistant prostate cancerInhibitorinhibitorinhibit

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