- ARV-825
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- $0.00 / 1mg
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2025-04-22
- CAS:1818885-28-7
- Min. Order: 1mg
- Purity: 98%min
- Supply Ability: 500mg
- ARV-825
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- $60.00 / 1mg
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2024-11-19
- CAS:1818885-28-7
- Min. Order:
- Purity: 98%
- Supply Ability: 10g
- ARV-825
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- $7.00 / 1KG
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2020-01-14
- CAS:1818885-28-7
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 100KG
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| | ARV-825 Basic information |
| Product Name: | ARV-825 | | Synonyms: | ARV-825;CS-2252;ARV-825;ARV 825;ARV825;AVR-825;6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[4-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-;Epigenetic Reader Domain,inhibit,PROTACs,ARV 825,Inhibitor,ARV825,ARV-825;2-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide;ARV-825, 10 mM in DMSO | | CAS: | 1818885-28-7 | | MF: | C46H47ClN8O9S | | MW: | 923.43 | | EINECS: | | | Product Categories: | | | Mol File: | 1818885-28-7.mol |  |
| | ARV-825 Chemical Properties |
| density | 1.47±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C(protect from light) | | solubility | DMSO:5.0(Max Conc. mg/mL);5.41(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);5.41(Max Conc. mM)
Water:0.0(Max Conc. mg/mL);0.0(Max Conc. mM) | | form | A crystalline solid | | pka | 10.74±0.40(Predicted) | | color | Light yellow to yellow |
| | ARV-825 Usage And Synthesis |
| Description | ARV-825 is a PROTAC molecule composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety. ARV-825 recruits BRD4 to E3 ubiquitin ligase cereblon, resulting in the degradation of BRD4. | | Uses | ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. | | Biological Activity | ARV-825 is a BRD4 inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, causing rapid, efficient and sustained degradation of BRD4 protein and sustained downregulation of MYC levels. | | in vivo | In the mouse model transplanted with human leukemia cells, the leukemia burden of the mice in the ARV-825 experimental group was significantly lower than that in the control group, and their survival time was also longer than that in the control group. | | target | | Target | Value | BRD4 BD2
(Cell-free assay) | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 28 nM(Kd) BRD4 BD1
(Cell-free assay) | 90 nM(Kd) |
| | References | [1] Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. DOI:10.1016/j.chembiol.2015.05.009 |
| | ARV-825 Preparation Products And Raw materials |
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