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 persistent downregulation of MYC levels.

 

Brand: BCM

 

Target: Epigenetic Reader Domain

 

Signaling Pathways: Chromatin/Epigenetic

 

In Vitro: ARV-825 more effectively suppresses c-MYC levels and downstream signaling than small molecule BRD4 inhibitors resulting in more effective cell proliferation inhibition and apoptosis induction in BL.In Burkitt's lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis.

 

In Vivo: In mouse models transplanted with human leukemia cells, the leukemia load of the ARV-825 experimental group was significantly lower than that of the control group, and their survival time was longer than that of the control group.

 

pKa: 10.74±0.40(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)OCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=C(C=C8)Cl)C  

 

InChIKey: RWLOGRLTDKDANT-TYIYNAFKSA-N  

 

InChI: InChI=1S/C46H47ClN8O9S/c1-26-27(2)65-46-39(26)41(29-7-9-30(47)10-8-29)50-35(42-53-52-28(3)54(42)46)25-38(57)49-31-11-13-32(14-12-31)64-24-23-63-22-21-62-20-19-61-18-17-48-34-6-4-5-33-40(34)45(60)55(44(33)59)36-15-16-37(56)51-43(36)58/h4-14,35-36,48H,15-25H2,1-3H3,(H,49,57)(H,51,56,58)/t35-,36?/m0/s1

 

Attribute
[Chem 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]	ARV-825; ARV825
[CAS No.]	1818885-28-7
[MDL No.]	MFCD29472237
[Formula]	C46H47ClN8O9S
[Molecular]	923.43
[Form]	A crystalline solid
[Storage]	Keep in dark place. Sealed in dry, 2-8°C

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