|2-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂卓-6-基)-N-(4-(2-(2-(2-(2-((2-(2,6-二氧代哌啶-3-基)-1,3-二氧代异吲哚啉-4-基)氨基)乙氧基)乙氧基)乙氧基)乙氧基)苯基)乙酰胺|CsnPharm

CAS No.: 1818885-28-7

ARV-825 Catalog No. CSN18046

Synonyms: Arv-825

ARV-825 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with K_ds values of 90nM and 28nM for affinity to BD1 and BD2.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述ARV-825 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with K_ds values of 90nM and 28nM for affinity to BD1 and BD2. ARV-825 led to a fast and efficient degradation of BRD4 at concentration ranging in 1-300nM in Namalwa and CA-46 cells and a dose-dependent degradation of BRD4 post 1-24h in Namalwa and Ramos cells exposure to 100nM ARV-825. Also, it led to a more significant c-MYC suppression than JQ1 or OTX015 by depletion of BRD4 by ARV-825 at different concentration (0.1, 0.3 and 1μM) or time point (2-24h), as well as a longer lasting effect after washout (6, 24h). Consistent with this downregulation of c-MYC, ARV-825 achieved a superior effect on suppression of BL cell proliferation and apoptosis induction compared with JQ1 or OTX015, including Namalwa, CA-46, Ramos and DAUDI cell lines^[1].
动物研究
剂量
Mice: 5 mg/kg^[2] (i.p.), 10 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[2] (i.p.), 10 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] Lu J, Qian Y, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.0829 mL
- 5.4146 mL
- 10.8292 mL
- 5 mM
- 0.2166 mL
- 1.0829 mL
- 2.1658 mL
- 10 mM
- 0.1083 mL
- 0.5415 mL
- 1.0829 mL

技术信息

CAS号

1818885-28-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C46H47ClN8O9S

运输

蓝冰

分子量

923.43

别名

Arv-825

溶解度

DMSO	100.0 mg/mL (108.3 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (3.2 mM)

动物实验配方

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