1949837-12-0
Chemical Structure
ARV-771
- CAS No.: 1949837-12-0
- Formula:C49H60ClN9O7S2
- Molecular Weight:986.64
IUPAC Name: (2S,4R)-1-((S)-2-(tert-butyl)-15-((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)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
InChIKey: PQOGZKGXGLHDGS-QQRWPDCKSA-N
SMILES: CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@H](C4=NN=C(N42)C)CC(NCCOCCCOCC(N[C@H](C(N5C[C@@H](C[C@H]5C(N[C@@H](C)C6=CC=C(C=C6)C7=C(C)N=CS7)=O)O)=O)C(C)(C)C)=O)=O
Biological Activity: ARV-771 is a BET PROTAC degrader, with Kd values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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ARV-771 | 99.82% | ARV-771 is a BET PROTAC degrader, with Kd values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research. | ||||||||||||||||||||
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ARV-771 (Standard) | ≥98% | ARV-771 (Standard) is the analytical standard of ARV-771 (HY-100972). This product is intended for research and analytical applications. ARV-771 is a BET PROTAC degrader, with Kd values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research. | ||||||||||||||||||||
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References
- [1]. Wang C, et al. Nanozyme-Mediated PROTACs Delivery for Targeted Protein Degradation and Ferroptosis Sensitization in Prostate Cancer. Angewandte Chemie (International ed. in English). 2026 May 04;65(19):e6657773.
- [2]. Raina K, et al. 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. [Content Brief]
