ARV-825 is a small-molecule degrader of BET proteins that has been shown to inhibit acute myeloid leukemia cell proliferation and induce apoptosis. It has also been demonstrated that ARV-825 may inhibit cell proliferation, induce apoptosis, and induce cell cycle arrest in vitro against a multiple myeloma cell line, and inhibit cell growth in vivo in a mouse xenograft.
| Cas No. | 1818885-28-7 |
|---|---|
| Purity | ≥99% |
| Formula | C46H47ClN8O9S |
| Formula Wt. | 923.44 |
| Chemical Name | 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-ylamino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide |
| IUPAC Name | 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-[4-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]phenyl]acetamide |
| Synonym | ARV825; SCHEMBL17162093; RWLOGRLTDKDANT-TYIYNAFKSA-N; BCP19950; CS-4776 |
| Solubility | DMSO (1 mg/mL), DMF (5 mg/mL). |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Piya S, Mu H, Bhattacharya S, et al. BETP degradation simultaneously targets acute myelogenous leukemia stem cells and the microenvironment. J Clin Invest. 2019 Feb 21;130. pii:120654. PMID: 30829648.
Lim SL, Damnernsawad A, Shyamsunder P, et al. Proteolysis targeting chimeric molecules as therapy for multiple myeloma: efficacy, biomarker and drug combinations. Haematologica. 2019 Jan 3. pii:haematol.2018.201483. PMID: 30606790.
Saenz DT, Fiskus W, Qian Y, et al. Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells. Leukemia. 2017 Sep;31(9):1951-1961. PMID: 28042144.
