AR antagonist 4

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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.

For research use only. We do not sell to patients.

AR antagonist 4 Chemical Structure

CAS No. : 2883447-45-6

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Description

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]

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].

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

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.

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].

MedChemExpress (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 Rats^a^[1]

Compound	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-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: C_max, maximum drug concentration; AUC_0-t, area under the curve between 0 and t h; T_1/2, terminal half-life; T_max, the time taken to reach C_max.Values are expressed as the mean, n = 3.

Molecular Weight

456.62

Formula

C₂₉H₃₆N₄O

CAS No.

2883447-45-6

SMILES

C[C@@]12[C@](CC=C2N3C=NC(C)=C3)([H])[C@@]4([H])[C@]([C@@]5(C(C[C@H](CC5)NC(C6=CC=NC=C6)=O)=CC4)C)([H])CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wang A, et al. Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer. J Med Chem. 2022 Sep 7. [Content Brief]

AR antagonist 4 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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