country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-153519

Copy Link Print Information

WWL0245

WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC₅₀ (<1 nM) than BRD2/3 and PLK1 ( DC₅₀>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4.

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。

CAS 番号: 2869057-11-2
分子式: C₄₅H₅₁N₁₁O₈
分子量:873.96

保管条件:

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

Data Sheet (274 KB)

WWL0245 構造式

CAS 番号: 2869057-11-2

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

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
- Cellular Effect
- 体外実験
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

IC₅₀ & Target^[1]

BRD4

1 nM (IC₅₀)

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	0.053 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
DU-145	IC₅₀	10 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-negative human castration resistant DU-145 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-negative human castration resistant DU-145 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
LNCaP	IC₅₀	0.021 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-positive harmone sensitive human LNCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-positive harmone sensitive human LNCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
MV4-11	IC₅₀	0.003 μM Compound: 12a; WWL0245	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
PC-3	IC₅₀	2.435 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-negative human castration resistant PC-3 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-negative human castration resistant PC-3 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
VCaP	IC₅₀	0.016 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]

体外実験

WWL0245 (0-1 μM; 96h) suppresses the proliferation of AR-positive prostate cancer cells with IC₅₀ values range from 0.0159 μM -10 μM. It shows greater antiproliferative activity to AR-positive cell lines VCaP, LNCaP, 22Rv1 with IC₅₀ values of 0.016 μM, 0.021 μM, 0.053 μM, respectively^[1].
WWL0245 (1 μM; 24 hours) results in the downregulation of BRD4 and c-Myc in a time-dependent manner in LNCaP, 22Rv1, VCaP cell lines and results in the decrease of BRD4 level and c-Myc level in a concentration-dependent manner in 22Rv1 and VCaP cell with DC50 of sub-nanomolar. But WWL0245 could also downregulate BRD4 level in DU145 cells but has negligible effects in c-Myc level^[1].
WWL0245 (100 nM-1 μM; 24 hours) suppresses the transcription of AR-regulated genes (PSA, TMPRSS2, ERG, FKBP5, BMPR1B) at various degrees^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HL60, SU-DHL-6, RS4;11, JURKAT, A2780, MDA-MB-468, BT549, LNCaP, 22Rv1, and VCaP cells
Concentration:

0 μM -10 μM
Incubation Time:

96 h
Result:

Inhibited HL60, SU-DHL-6, RS4;11, JURKAT, A2780, MDA-MB-468, BT549, LNCaP, 22Rv1, and VCaP growth with IC₅₀ values of 0.0961, 0.0734, 0.0247, 0.5018, 0.0153, 0.2460, and 0.1732 μM, respcetively[1].

Western Blot Analysis^[1]

Cell Line:

Prostate cancer cell lines: LNCaP, 22Rv1, VCaP, DU145
Concentration:

1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time:

1 hour, 2 hours, 4 hours,12 hours, 24 hours,48 hours
Result:

Resulted in the downregulation of BRD4 and c-Myc in a time/concentration-dependent manner in 22Rv1 and VCaP cells.

RT-PCR^[1]

Cell Line:

Prostate cancer: VCaP cell
Concentration:

100 nM-1 μM
Incubation Time:

24 h
Result:

Suppressed the expression of AR-regulated genes in prostate cancer.

化学情報

CAS 番号 2869057-11-2
分子量 873.96
分子式 C₄₅H₅₁N₁₁O₈
SMILES

CC[C@@H](N(C1=N2)CC3CCCCC3)C4=NN=C(C)N4C1=CN=C2NC5=C(C=C(C=C5)C(NC6CCN(CC6)C(COC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8=O)=O)=CC=C7)=O)=O)OC
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]. Rong Hu, et al. Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor. Eur J Med Chem. 2022 Jan 5;227:113922. [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.

Keywords

MOQ

Minimum order quantity

100 mg

お問い合わせ在庫あり

Other size

お問い合わせ

Amount: USD 0.00

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

製品名:
製品番号:
数量:
日本の代理先をお選びください:

製品名:
CAS 番号:
生物種:
純度:
数量:

WWL0245

Epigenetic Reader Domain 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

WWL0245 関連分類

HY-153519 関連分類