1. PROTAC Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor PROTACs
  3. ARD-1676

ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models.
(Pink: Androgen Receptor ligand (HY-150878); Blue: Cereblon ligand (HY-W248665); Black: linker).

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ARD-1676

ARD-1676 構造式

CAS 番号 : 2632305-36-1

容量 価格(税別) 在庫状況 数量
5 mg $850 在庫あり
10 mg $1430 在庫あり
25 mg $3000 在庫あり
50 mg $4800 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models[1]. (Pink: Androgen Receptor ligand (HY-150878); Blue: Cereblon ligand (HY-W248665); Black: linker).

Cellular Effect
Cell Line Type Value Description References
LNCaP IC50
2.8 nM
Compound: 39; ARD-1676
Growth inhibition in human LNCaP cells assessed as reduction in cell viability
Growth inhibition in human LNCaP cells assessed as reduction in cell viability
[PMID: 37683104]
VCaP IC50
11.5 nM
Compound: 39; ARD-1676
Growth inhibition in human VCaP cells
Growth inhibition in human VCaP cells
[PMID: 37683104]
体外実験

The DC50 values of ARD-1676 for AR degradation in AR+ VCaP and LNCaP cell lines are 0.1 and 1.1 nM, respectively, and the IC50 values in VCaP and LNCaP cell lines are 11.5 and 2.8 nM respectively[1].

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

体内実験

The oral bioavailability of ARD-1676 was 67%, 44%, 31%, and 99% in mice, rats, dogs, and monkeys, respectively. ARD-1676 effectively reduces AR protein levels in mouse VCaP tumor tissues and inhibits tumor growth in VCaP mouse xenograft tumor models[1].

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

分子量

788.33

分子式

C44H46ClN7O5

CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

C[C@H]1CC2(CN1C3=CC=C(C(Cl)=C3)C#N)CCN(CC2)C4=CC=C(C=C4)C(N5CCC(CC5)CN6CC7=C(C6)C=C8C(N(C(C8=C7)=O)C9CCC(NC9=O)=O)=O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (126.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2685 mL 6.3425 mL 12.6850 mL
5 mM 0.2537 mL 1.2685 mL 2.5370 mL
10 mM 0.1269 mL 0.6343 mL 1.2685 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます:C1V1 = C2V2

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純度とドキュメンテーション

純度: 99.36%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2685 mL 6.3425 mL 12.6850 mL 31.7126 mL
5 mM 0.2537 mL 1.2685 mL 2.5370 mL 6.3425 mL
10 mM 0.1269 mL 0.6343 mL 1.2685 mL 3.1713 mL
15 mM 0.0846 mL 0.4228 mL 0.8457 mL 2.1142 mL
20 mM 0.0634 mL 0.3171 mL 0.6343 mL 1.5856 mL
25 mM 0.0507 mL 0.2537 mL 0.5074 mL 1.2685 mL
30 mM 0.0423 mL 0.2114 mL 0.4228 mL 1.0571 mL
40 mM 0.0317 mL 0.1586 mL 0.3171 mL 0.7928 mL
50 mM 0.0254 mL 0.1269 mL 0.2537 mL 0.6343 mL
60 mM 0.0211 mL 0.1057 mL 0.2114 mL 0.5285 mL
80 mM 0.0159 mL 0.0793 mL 0.1586 mL 0.3964 mL
100 mM 0.0127 mL 0.0634 mL 0.1269 mL 0.3171 mL
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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Help & FAQs
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    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.

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Inquiry Information

製品名:
ARD-1676
製品番号:
HY-156111
数量:
MCE 日本正規代理店: