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ARV-825

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Chemical Structure| 1818885-28-7 同义名 : -
CAS号 : 1818885-28-7
货号 : A370626
分子式 : C46H47ClN8O9S
纯度 : 99%+
分子量 : 923.432
MDL号 : MFCD29472237
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(54.15 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BET

    BRD4 BD2, Kd:28 nM

    BRD4 BD1, Kd:90 nM
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 Kds 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.08mL

0.22mL

0.11mL

5.41mL

1.08mL

0.54mL

10.83mL

2.17mL

1.08mL
参考文献

[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.