ARV-771 manufacturers
- ARV-771
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- $0.00 / 1mg
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2026-02-26
- CAS:1949837-12-0
- Min. Order: 1mg
- Purity: 98%min
- Supply Ability: 500mg
- ARV-771
-
- $55.00 / 1mg
-
2026-01-25
- CAS:1949837-12-0
- Min. Order:
- Purity: 99.69%
- Supply Ability: 10g
- ARV-771
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- $0.00 / 100MG
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2025-03-16
- CAS:1949837-12-0
- Min. Order: 1MG
- Purity: 98
- Supply Ability: 100G
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| | ARV-771 Basic information |
| Product Name: | ARV-771 | | Synonyms: | ARV-771;ARV 771; ARV771;(2S,4R)-1-[(2S)-2-[[2-[3-[2-[[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]acetyl]amino]ethoxy]propoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide;(2S,4R)-1-[(2S)-2-[[2-[3-[2-[[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]acetyl]amino]ethoxy]propoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-;(2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-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-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide;Epigenetic Reader Domain,ARV-771,ARV771,inhibit,ARV 771,PROTACs,Inhibitor;ARV-771, 10 mM in DMSO;(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-diazapentadecan-1-oyl]-4-hydroxy-N-[(S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]pyrrolidine-2-carboxamide | | CAS: | 1949837-12-0 | | MF: | C49H60ClN9O7S2 | | MW: | 986.65 | | EINECS: | | | Product Categories: | ADC LINKER;API | | Mol File: | 1949837-12-0.mol |  |
| | ARV-771 Chemical Properties |
| density | 1.39±0.1 g/cm3(Predicted) | | storage temp. | Sealed in dry,Store in freezer, under -20°C | | solubility | DMSO:65.92(Max Conc. mg/mL);68.22(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);20.7(Max Conc. mM)
DMF:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.14(Max Conc. mM)
Ethanol:55.0(Max Conc. mg/mL);56.92(Max Conc. mM) | | pka | 13.61±0.46(Predicted) | | form | A crystalline solid | | color | White to light yellow | | InChI | InChI=1/C49H60ClN9O7S2/c1-27-30(4)68-48-41(27)42(33-14-16-35(50)17-15-33)54-37(45-57-56-31(5)59(45)48)23-39(61)51-18-21-65-19-9-20-66-25-40(62)55-44(49(6,7)8)47(64)58-24-36(60)22-38(58)46(63)53-28(2)32-10-12-34(13-11-32)43-29(3)52-26-67-43/h10-17,26,28,36-38,44,60H,9,18-25H2,1-8H3,(H,51,61)(H,53,63)(H,55,62)/t28-,36+,37-,38-,44+/s3 | | InChIKey | PQOGZKGXGLHDGS-BZTQNJCZNA-N | | SMILES | [s]1cnc(c1c2ccc(cc2)[C@@H](NC(=O)[C@H]3N(C[C@@H](C3)O)C(=O)[C@@H](NC(=O)COCCCOCCNC(=O)C[C@@H]4N=C(c6c([s]c(c6C)C)[n]7c4nnc7C)c5ccc(cc5)Cl)C(C)(C)C)C)C | | SMILES | CC1=C(SC2N3C(=NN=C3[C@H](CC(=O)NCCOCCCOCC(=O)N[C@@H](C(C)(C)C)C(N3C[C@H](O)C[C@H]3C(=O)N[C@H](C3C=CC(C4=C(N=CS4)C)=CC=3)C)=O)N=C(C3C=CC(Cl)=CC=3)C1=2)C)C |&1:10,26,34,37,41,r| |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | ARV-771 Usage And Synthesis |
| Description | ARV-771 is a BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2), respectively. | | Uses | ARV-771 is an effective BET degrader of the PROTAC class. | | Biological Functions | ARV-771, a von Hippel–Landau (VHL) E3 ligase-based BET PROTAC, is highly active against cellular models of CRPC. ARV-771 in these cells results in rapid BET protein degradation with DC50 (the drug concentration that results in 50% protein degradation) values <1 nM. Interestingly, ARV–771–mediated BET degradation leads to decreased both FL-AR and AR-V7 at the transcript level. In contrast, treating CRPC cells with BET inhibitors leads to the suppression of AR-V7 but not of FL-AR levels. Moreover, ARV-771 causes significantly greater apoptotic cell death than a BET inhibitor. ARV-771 dramatically suppresses the proliferation of castration-resistant prostate cancer models via inducing Von Hippel Lindau (VHL) E3 ligase-mediated degradation of BRDs and inhibiting AR signaling. A subsequent study has demonstrated that ARV-771 can also suppress the proliferation of mantle cell lymphoma cells via increasing the levels of tumour suppressors, including CDKN1A/p21, HEXIM1, and NOXA[1].
| | Biological Activity | ARV-771 is a potent pan-(bromodomain and extra-terminal) BET degrader, a novel BET-PROTAC (proteolysis-targeting chimera), for BRD2(1), BRD2(2), BRD3(1) The Kd values of , BRD3(2), BRD4(1) and BRD4(2) were 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM and 7.6 nM, respectively. | | target | | Target | Value | BRD2-BD2
(Cell-free assay) | 4.7 nM(Kd) | BRD3-BD2
(Cell-free assay) | 7.6 nM(Kd) | td> BRD4-BD2
(Cell-free assay) | 7.6 nM(Kd) | BRD3-BD1
(Cell-free assay) | 8.3 nM(Kd) | BRD4-BD1
(Cell-free assay) | 9.6 nM(Kd) |
| | storage | Store at -20°C | | References | [1] Yuanfei Deng. “ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression.” Frontiers in Pharmacology (2022).
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| | ARV-771 Preparation Products And Raw materials |
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