ARV-771

製品コードS8532 バッチS853201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₄₉H₆₀ClN₉O₇S₂

分子量

986.64

CAS No.

1949837-12-0

Solubility (25°C)*

体外

DMSO

100 mg/mL (101.35 mM)

Ethanol

100 mg/mL (101.35 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
in vitro	ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. Treatment of CRPC cells with this compound results in apoptosis.^[1]
in vivo	ARV-771 induces degradation in vivo. This compound results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	22Rv1 cells, VCaP cells, LnCaP95 cells
	濃度	1-300 nM
	反応時間	24 h, 72 h
	実験の流れ	c-MYC ELISA. 22Rv1 cells (30,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. AR ELISA. VCaP cells (40,000 cells per well) were dosed with this compound serially diluted at 1:3 ratio for an eight-point dose curve. Cell Proliferation Assay Protocol. 22Rv1 cells (5,000 cells per well) were dosed with this chemical serially diluted 1:3 for a 10-point dose curve for 72 h.
動物実験	動物モデル	Mice implanted subcutaneously with 5 × 10⁶ 22Rv1 or VCaP cells
	投薬量	30 mg/kg
	投与方法	IH/SC

参考

https://pubmed.ncbi.nlm.nih.gov/27274052/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471]	PubMed: 38508142
Characterization of the BH1406 non-small cell lung cancer (NSCLC) cell line carrying an activating SOS1 mutation [ Transl Lung Cancer Res, 2024, 13(11):2987-2997]	PubMed: 39670010
BET Bromodomain Degradation Disrupts Function but Not 3D Formation of RNA Pol2 Clusters [ Pharmaceuticals (Basel), 2023, 16(2)199]	PubMed: 37259348
ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression [ Front Pharmacol, 2022, 13:858901]	PubMed: 35600879

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。