ARV-825 _BRD4 PROTAC Degrader - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEARV-825Cat. No.: HY-16954CAS No.: 1818885-28-7分式: CHClNOS分量: 923.43作靶點(diǎn): Epigenetic Reader Domain; PROTAC作通路: Epigenetics; PROTAC儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (54.

2、15 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.0829 mL 5.4146 mL 10.8292 mL5 mM 0.2166 mL 1.0829 mL 2.1658 mL10 mM 0.1083 mL 0.5415 mL 1.0829 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠

3、性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.71 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.71 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChe

4、mEBIOLOGICAL ACTIVITY物活性 ARV-825種 PROTAC 類的 BRD4 抑制劑。ARV-825 對 BRD4 的 BD1 和 BD2 結(jié)構(gòu)域具有親和，Kd 值分別為 90 和 28 nM。IC50 & Target Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4) 1體外研究 ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3ubiquiti

5、n ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficientdegradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825have Kds of 28-90 nM and 3 M to their respective targets, this suggests that ARV-825 acts in asubst

6、oichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors 1.PROTOCOLKinase Assay 1 Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscanby

7、DiscoverX 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Clin Cancer Res. 2019 Jun 1;25(11):3404-3416. Sci Rep. 2018 Sep 5;8(1):13225.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.McePdfHeightCaution: Product has not been fully validated for medical applications.For resear