ARV-825

製品コードS8297 バッチS829703

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₄₆H₄₇ClN₈O₉S

分子量

923.43

CAS No.

1818885-28-7

Solubility (25°C)*

体外

DMSO

100 mg/mL (108.29 mM)

Ethanol

4 mg/mL (4.33 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (5.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
in vitro	Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines^[1]. The IC50s of this compound for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). This treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena^[3].
in vivo	In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice^[3].

製品説明

ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.

in vitro

Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines^[1].

The IC50s of this compound for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). This treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena^[3].

in vivo

In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	RS4;11 cells
	濃度	3, 10, 30 nM
	反応時間	3 h
	実験の流れ	RS4;11 cells are treated for 3 h with this compound at indicated concentrations, and proteins are probed by specific antibodies.
動物実験	動物モデル	NOD/SCID gamma mice
	投薬量	5 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/26051217/
https://pubmed.ncbi.nlm.nih.gov/28339196/
http://www.bloodjournal.org/content/128/22/748?sso-checked=true

https://pubmed.ncbi.nlm.nih.gov/30903020/

+ 展开

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：

Single-cell analysis of neoplastic plasma cells identifies myeloma pathobiology mediators and potential targets [ Cell Rep Med, 2025, S2666-3791(24)00696-7]	PubMed: 39855192
Single-cell morphology encodes functional subtypes of senescence in aging human dermal fibroblasts [ Sci Adv, 2025, 11(17):eads1875]	PubMed: 40279419
Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]	PubMed: 38262581
Single-cell morphology encodes functional subtypes of senescence in aging human dermal fibroblasts [ bioRxiv, 2024, 2024.05.10.593637]	PubMed: 38798365
Pharmacological inhibition of bromodomain and extra-terminal proteins induces an NRF-2-mediated antiviral state that is subverted by SARS-CoV-2 infection [ PLoS Pathog, 2023, 19(9):e1011657]	PubMed: 37747932
FET fusion oncoproteins interact with BRD4 and SWI/SNF chromatin remodelling complex subtypes in sarcoma [ Mol Oncol, 2022, 10.1002/1878-0261.13195]	PubMed: 35182012
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921]	PubMed: 35758684
Protein Ligand Interactions Using Surface Plasmon Resonance [ Methods Mol Biol, 2021, 2365:3-20]	PubMed: 34432236
Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. [ J Exp Clin Cancer Res, 2019, 38(1):383]	PubMed: 31470872

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。

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