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AR antagonist 4

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.

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No. CAS: 2883447-45-6
Fòrmula: C₂₉H₃₆N₄O
Peso molecular:456.62

Almacenamiento:

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

Data Sheet (275 KB)

AR antagonist 4 Chemical Structure

No. CAS: 2883447-45-6

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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]

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	590 nM Compound: 67-b	Antiproliferative activity against human 22Rv1 cells expressing AR-v7 assessed as reduction in cell viability measured after 6 days by CTG assay Antiproliferative activity against human 22Rv1 cells expressing AR-v7 assessed as reduction in cell viability measured after 6 days by CTG assay	[PMID: 36070471]
LNCaP	IC₅₀	205.1 nM Compound: 67-b	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay	[PMID: 36070471]

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.

Chemical Information

No. CAS 2883447-45-6
Peso molecular 456.62
Fòrmula C₂₉H₃₆N₄O
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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