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製品番号: HY-176128

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BWA-6047

BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer.
(Pink: Androgen Receptor ligand (HY-176129); Blue: Cereblon ligand (HY-W069604); Black: linker (HY-B0236)).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₄₂H₄₆ClN₅O₇
分子量:768.30

保管条件:

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

Data Sheet (274 KB)

BWA-6047 構造式

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer^[1]. (Pink: Androgen Receptor ligand (HY-176129); Blue: Cereblon ligand (HY-W069604); Black: linker (HY-B0236)).

IC₅₀ & Target^[1]

Cereblon

PARP-1

Caspase 3

PROTACs アイソフォーム固有の製品をすべて表示 :

PARP アイソフォーム固有の製品をすべて表示 :

Caspase アイソフォーム固有の製品をすべて表示 :

体外実験

BWA-6047 (0.01-300 μM; 2-36 h) dose- and time-dependently degrades AR, AR-V7, and GSPT1 in LNCaP, VCaP, and 22Rv1 prostate cancer cells via a CRBN- and proteasome-dependent mechanism (DC₅₀ = 0.6-15.6 nM), with potent activity even in Enzalutamide (HY-70002)-resistant cells^[1].
BWA-6047 (0.01-1000000 nM; 72 h) potently inhibits the proliferation of AR-dependent prostate cancer cells, including Enzalutamide-resistant lines, with low activity against AR-independent cancer cells and normal cells^[1].
BWA-6047 (0.01-100000 nM; 24 h) potently inhibits the transcriptional activity of wild-type and Enzalutamide-resistant AR mutants (AR^W741L, AR^F876L) in 293T cells^[1].
BWA-6047 (1-100 nM; 24 h) suppresses the expression of AR downstream target genes (PSA, TMPRSS2, FKBP5) in 22Rv1 and LNCaP prostate cancer cells^[1].
BWA-6047 (1-30 nM; 24 h) induces G1 phase cell cycle arrest in 22Rv1 prostate cancer cells in a dose-dependent manner^[1].
BWA-6047 (1-100 nM; 24 h) induces apoptosis in 22Rv1 and LNCaP prostate cancer cells, as evidenced by increased levels of cleaved apoptotic markers^[1].
BWA-6047 (30 nM; 12 h) promotes the polyubiquitination of AR and GSPT1 in 22Rv1 prostate cancer cells, a key step in proteasomal degradation^[1].

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

Real Time qPCR^[1]

Cell Line:

22Rv1 and LNCaP prostate cancer cells
Concentration:

1, 3 nM (22Rv1 cells); 10, 30, 100 nM (LNCaP cells)
Incubation Time:

24 h
Result:

Significantly decreased mRNA levels of PSA, TMPRSS2, and FKBP5 at 1 nM and 3 nM in 22Rv1 cells.
Significantly decreased mRNA levels of PSA, TMPRSS2, and FKBP5 at 10 nM, 30 nM, and 100 nM in LNCaP cells.

Cell Cycle Analysis^[1]

Cell Line:

22Rv1 prostate cancer cells
Concentration:

1, 3, 10, 30 nM
Incubation Time:

24 h
Result:

Increased G1 phase proportion from 49.7% (control) to 56.3% (1 nM), 55.6% (3 nM), 58.9% (10 nM), and 74.6% (30 nM) in 22Rv1 cells.
Decreased corresponding S phase proportion from 41.4% to 34.1%, 36.6%, 33.4%, and 22.3% in 22Rv1 cells.

Western Blot Analysis^[1]

Cell Line:

22Rv1 and LNCaP prostate cancer cells
Concentration:

1, 3, 10, 30 μM (22Rv1 cells); 1, 3, 10, 30, 100 μM (LNCaP cells)
Incubation Time:

24 h
Result:

Induced dose-dependent increases in cleaved-PARP-1 and cleaved-caspase-3 levels in 22Rv1 cells.
Induced dose-dependent increases in cleaved-PARP-1 and cleaved-caspase-3 levels in LNCaP cells.

Parmacokinetics

Species	Dose	Route	C_max	AUC	F	T_1/2	CL
Mice^[1]	2 mg/kg	i.v.	1121 ng/mL	1850 ng·h/mL	/	0.9 h	1081 mL/h/kg
Mice^[1]	10 mg/kg	p.o.	206 ng/mL	1035 ng·h/mL	11.2 %	/	/

体内実験

BWA-6047 (20 mg/kg; p.o.; daily; 26 days) achieves 60.0% tumor growth inhibition in castrated male NOD SCID mice bearing LNCaP xenografts, with significant reductions in intratumoral AR, GSPT1, and serum PSA, and no apparent toxicity^[1].

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

Animal Model:

NOD SCID mice bearing LNCaP xenografts (male, 6 weeks old, castrated after tumor reached ~180 mm³)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 26 days
Result:

Achieved 60.0% tumor growth inhibition (TGI) relative to the vehicle control.
Significantly reduced intratumoral levels of androgen receptor (AR) and G1 to S phase transition 1 (GSPT1) proteins compared to the vehicle control.
Significantly reduced serum prostate-specific antigen (PSA) concentrations compared to the vehicle control.
Showed no observable weight loss in treated mice.

化学情報

分子量 768.30
分子式 C₄₂H₄₆ClN₅O₇
SMILES

O=C(CCCCCNC1=CC=C2C(N(C3C(NC(CC3)=O)=O)C(C2=C1)=O)=O)N4CCC(CC4)COC5=C(C#N)C=C(C(C)(C6=CC=C(C=C6)OC)C)C=C5Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Zhang B, et al. Rational Design of Dual Degraders by Incorporating Molecular Glue Structural Features into PROTAC Degraders. J Med Chem. 2025;68(10):10268-10298. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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BWA-6047

PROTACs アイソフォーム固有の製品をすべて表示

PARP アイソフォーム固有の製品をすべて表示

Caspase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

BWA-6047 関連分類

HY-176128 関連分類