ARV-771
ARV-771 is a small-molecule pan-BET degrader. ARV-771 demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. Unlike BET inhibitors, ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.
For research use only. We do not sell to patients.
Chemical Information
| Name | ARV-771 |
|---|---|
| Iupac Chemical Name | (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)ethyl)pyrrolidine-2-carboxamide |
| Synonyms | ARV-771; ARV 771; ARV771. |
| Molecular Formula | C50H63N9O7S2 |
| Molecular Weight | 966.23 |
| Smile | 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 |
| InChiKey | HJGNHEQIOZDQRW-VZRXUJQISA-N |
| 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/h11-18,27,30,37-39,45,60H,10,19-26H2,1-9H3,(H,51,61)(H,53,63)(H,55,62)/t30-,37+,38-,39-,45+/m0/s1 |
| CAS Number | 1949837-12-0 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Purity | 98% Min. |
|---|---|
| Handling | |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi AM, Wang J, Chen X, Dong H,
Siu K, Winkler JD, Crew AP, Crews CM, Coleman KG. PROTAC-induced BET protein
degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad
Sci U S A. 2016 Jun 28;113(26):7124-9. doi: 10.1073/pnas.1521738113. Epub 2016
Jun 6. PubMed PMID: 27274052; PubMed Central PMCID: PMC4932933.
2: Saenz DT, Fiskus W, Qian Y, Manshouri T, Rajapakshe K, Raina K, Coleman KG,
Crew AP, Shen A, Mill CP, Sun B, Qiu P, Kadia TM, Pemmaraju N, DiNardo C, Kim MS,
Nowak AJ, Coarfa C, Crews CM, Verstovsek S, Bhalla KN. Novel BET protein
proteolysis-targeting chimera exerts superior lethal activity than bromodomain
inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML
cells. Leukemia. 2017 Jan 31. doi: 10.1038/leu.2016.393. [Epub ahead of print]
PubMed PMID: 28042144.
Chemical Structure
