ARV-825

製品コードS8297 バッチS829701

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	3 mg/mL (3.24 mM)
		Water	Insoluble
* <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は、BRD4をE3ユビキチンリガーゼセレブロンにリクルートするBRD4阻害剤であり、BRD4の迅速かつ効率的で持続的な分解とMYCの持続的な下方制御をもたらします。
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. 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.
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.

製品説明

ARV-825は、BRD4をE3ユビキチンリガーゼセレブロンにリクルートするBRD4阻害剤であり、BRD4の迅速かつ効率的で持続的な分解とMYCの持続的な下方制御をもたらします。

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.

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.

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.

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/

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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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