ARV-825
ARV-825是一种BRD4抑制剂，可招募BRD4到E3泛素连接酶cereblon上，引起BRD4蛋白快速、有效和持续的降解，持续性下调MYC水平。
ARV-825 Chemical Structure
CAS: 1818885-28-7
产品质控
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| RS4:11 | Function assay | 3 to 30 nM | 3 hrs | Induction of cereblon/cullin 4A-mediated BRD2 degradation in human RS4:11 cells at 3 to 30 nM after 3 hrs by Western blot method | 28339196 |
| RS4:11 | Function assay | 3 to 30 nM | 3 hrs | Induction of cereblon/cullin 4A-mediated BRD3 degradation in human RS4:11 cells at 3 to 30 nM after 3 hrs by Western blot method | 28339196 |
| RS4:11 | Function assay | 3 to 30 nM | 3 hrs | Induction of cereblon/cullin 4A-mediated BRD4 degradation in human RS4:11 cells at 3 to 30 nM after 3 hrs by Western blot method | 28339196 |
| 22RV1 | Function assay | 24 hrs | Induction of CRBN-mediated BRD4 degradation in human 22RV1 cells measured after 24 hrs by immunoblotting analysis, DC50 = 0.00057 μM. | 30684871 | |
| NAMALWA | Function assay | overnight | Protac activity at Cereblon/BRD4 in human NAMALWA cells assessed as induction of BRD4 protein degradation in human NAMALWA cells after overnight incubation by immunoblot method, DC50 = 0.001 μM. | 31047748 | |
| CA46 | Function assay | overnight | Protac activity at Cereblon/BRD4 in human CA46 cells assessed as induction of BRD4 protein degradation in human CA46 cells after overnight incubation by immunoblot analysis, DC50 = 0.001 μM. | 31047748 | |
| MV4-11 | Growth inhibition assay | 96 hrs | Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay, IC50 = 0.00105 μM. | 30019901 | |
| RS4:11 | Cytotoxicity assay | 4 days | Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay, IC50 = 0.0033 μM. | 28339196 | |
| RS4:11 | Growth inhibition assay | 96 hrs | Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay, IC50 = 0.0033 μM. | 30019901 | |
| MV4-11 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay, EC50 = 0.01698 μM. | 28595007 | |
| MOLM13 | Cytotoxicity assay | 4 days | Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay, IC50 = 0.0182 μM. | 28339196 | |
| MOLM13 | Growth inhibition assay | 96 hrs | Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay, IC50 = 0.0182 μM. | 30019901 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay, EC50 = 0.03467 μM. | 28595007 | |
| U266 | Function assay | 12 hrs | Induction of CRBN-mediated BRD4 degradation in human U266 cells up to 1000 nM measured after 12 hrs by immunoblotting analysis | 30684871 | |
| U266 | Function assay | 12 hrs | Induction of CRBN ubiquitin ligase-mediated IKZF1 degradation in human U266 cells up to 1000 nM measured after 12 hrs by immunoblotting analysis | 30684871 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | ARV-825是一种BRD4抑制剂，可招募BRD4到E3泛素连接酶cereblon上，引起BRD4蛋白快速、有效和持续的降解，持续性下调MYC水平。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 与其他BRD4抑制剂比较，在伯基特氏淋巴瘤细胞中，ARV-825的处理可引起c-MYC水平和下游细胞增殖和凋亡诱导发生更为显著的变化[1]。 与ARV-825共孵育72小时，ARV-825对所检测细胞系和原代AML细胞的IC50值在2-50 nM范围内。在AML细胞中，ARV-825可降低PIM1水平和CXCR4的磷酸化水平，而PIM1或CXCR4的过表达可逆转该效应[3]。 |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | RS4;11细胞 | ||
| 浓度 | 3, 10, 30 nM | |||
| 孵育时间 | 3 h | |||
| 方法 | 用一定浓度范围的化合物处理RS4;11细胞，孵育3小时。然后提取细胞蛋白，用特定抗体检测蛋白表达水平。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | BRD1 / BRD2 / BRD3 / BRD4 / p21 c-MYC PARP / cleaved PARP CDK6 / CDK4 cleaved caspase 9 / cleaved caspase 3 Akt / pAKT-S473 / mTOR / p-mTOR-S2448 / p70S6K / p70S6K-T389 / 4EBP1/ p-4EBP1-S65 / PDK1 / p-PDK1-S241 / PI3K / p-PI3K-T458 JAK2 / p-STAT5 / p-STAT3 / PIM1 / p27 / Bcl-xl / γH2AX |
|
30903020 | |
| Immunofluorescence | BRD4 |
|
28042144 | |
| Growth inhibition assay | Cell viability |
|
26051217 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在移植有人源白血病细胞的小鼠模型中，ARV-825实验组的小鼠的白血病负荷显著低于对照组，其生存时间也较对照组长[3]。 |
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|---|---|---|
化学信息&溶解度
| 分子量 | 923.43 | 分子式 | C46H47ClN8O9S |
| CAS号 | 1818885-28-7 | SDF | -- |
| Smiles | CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)OCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=C(C=C8)Cl)C | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
DMSO : 100 mg/mL ( (108.29 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 6 mg/mL (6.49 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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