For research use only. Not for therapeutic Use.
ARV-771(CAT: I001969) is a small-molecule pan-BET degrader. It is designed to target and degrade bromodomain and extra-terminal (BET) proteins, including BRD2, BRD3, and BRD4. BET proteins are involved in the regulation of gene expression, and their dysregulation has been implicated in various diseases, including cancer. ARV-771 works by binding to BET proteins and promoting their degradation, leading to the inhibition of oncogenic transcriptional programs. This mechanism of action makes ARV-771 a potential therapeutic agent for the treatment of cancer and other diseases where BET proteins play a role.
| Catalog Number | I001969 |
| CAS Number | 1949837-12-0 |
| Synonyms | ARV-771; ARV 771; ARV771.;(2S,4R)-1-((S)-2-(tert-butyl)-4,14-dioxo-15-((S)-2,3,9-trimethyl-4-(p-tolyl)-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)et |
| Molecular Formula | C50H63N9O7S2 |
| Purity | ≥95% |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4°Cfor short term (days to weeks), or -20 °C for long term (months). |
| IC50 | Kd: 4.7 (BRD 2), 7.6 (BRD 3), 7.6 nM (BRD 4) |
| InChI | InChI=1S/C50H63N9O7S2/c1-28-11-13-35(14-12-28)43-42-29(2)32(5)68-49(42)59-33(6)56-57-46(59)38(54-43)24-40(61)51-19-22-65-20-10-21-66-26-41(62)55-45(50(7,8)9)48(64)58-25-37(60)23-39(58)47(63)53-30(3)34-15-17-36(18-16-34)44-31(4)52-27-67-44/h11-18,27,30,37- |
| InChIKey | HJGNHEQIOZDQRW-VZRXUJQISA-N |
| SMILES | CC1=C(C)C(C(C2=CC=C(C)C=C2)=N[C@H]3CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=O)=C(S1)N7C3=NN=C7C |
| Reference | 1: Saenz DT, Fiskus W, Qian Y, Manshouri T, Rajapakshe K, Raina K, Coleman KG, 2: Sun B, Fiskus W, Qian Y, Rajapakshe K, Raina K, Coleman KG, Crew AP, Shen A, 3: Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi AM, Wang J, Chen X, Dong H, |
