ARV-825

目錄號：S8297 Purity: 99.45%

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

CAS: 1818885-28-7

規(guī)格	價格	庫存
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
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.45%

99.45

ARV-825相關(guān)產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息(PMID)
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

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胞中，ARV-825的處理可引起c-MYC水平和下游細胞增殖和凋亡誘導(dǎo)發(fā)生更為顯著的變化^[1]。與ARV-825共孵育72小時，ARV-825對所檢測細胞系和原代AML細胞的IC50值在2-50 nM范圍內(nèi)。在AML細胞中，ARV-825可降低PIM1水平和CXCR4的磷酸化水平，而PIM1或CXCR4的過表達可逆轉(zhuǎn)該效應(yīng)^[3]。
細胞實驗	細胞系	RS4;11細胞
	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細胞，孵育3小時。然后提取細胞蛋白，用特定抗體檢測蛋白表達水平。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	BRD1 / BRD2 / BRD3 / BRD4 / p21 c-MYC PARP / cleaved PARP CDK6 / CDK4 cleaved caspase 9 / cleaved caspase 3