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ARV-825

ARV-825是一種BRD4抑制劑，可招募BRD4到E3泛素連接酶cereblon上，引起B(yǎng)RD4蛋白快速、有效和持續(xù)的降解，持續(xù)性下調(diào)MYC水平。

ARV-825 Chemical Structure

ARV-825 Chemical Structure

CAS: 1818885-28-7

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 2039.31 現(xiàn)貨
2mg 876.78 現(xiàn)貨
5mg 1614.35 現(xiàn)貨
25mg 4480.34 現(xiàn)貨
100mg 10401.52 現(xiàn)貨
1g 23900 現(xiàn)貨
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ARV-825相關(guān)產(chǎn)品

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 ARV-825是一種BRD4抑制劑，可招募BRD4到E3泛素連接酶cereblon上，引起B(yǎng)RD4蛋白快速、有效和持續(xù)的降解，持續(xù)性下調(diào)MYC水平。
靶點(diǎn)
BRD4 BD2 [1]
(Cell-free assay)		 BRD4 BD1 [1]
(Cell-free assay)
28 nM(Kd) 90 nM(Kd)
體外研究(In Vitro)
體外研究活性

與其他BRD4抑制劑比較，在伯基特氏淋巴瘤細(xì)胞中，ARV-825的處理可引起c-MYC水平和下游細(xì)胞增殖和凋亡誘導(dǎo)發(fā)生更為顯著的變化[1]。

與ARV-825共孵育72小時，ARV-825對所檢測細(xì)胞系和原代AML細(xì)胞的IC50值在2-50 nM范圍內(nèi)。在AML細(xì)胞中，ARV-825可降低PIM1水平和CXCR4的磷酸化水平，而PIM1或CXCR4的過表達(dá)可逆轉(zhuǎn)該效應(yīng)[3]。
細(xì)胞實驗 細(xì)胞系 RS4;11細(xì)胞
濃度 3, 10, 30 nM
孵育時間 3 h
方法

用一定濃度范圍的化合物處理RS4;11細(xì)胞，孵育3小時。然后提取細(xì)胞蛋白，用特定抗體檢測蛋白表達(dá)水平。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot

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