CAS No. 1949837-12-0
| IUPAC Name | (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 | |
|---|---|---|
| CAS Number | 1949837-12-0 | |
| Molecular Formula |
C49H60ClN9O7S2 |
|
| Molecular Weight (MW) | 986.64 | |
| SMILES | CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NC(C)C5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)C7=CC=C(C=C7)Cl)C | |
| InChIKey | PQOGZKGXGLHDGS-QQRWPDCKSA-N |
ARV-771 is a potent pan-bromodomain and extra-terminal (BET) degrader that targets BET proteins including BRD2, BRD3, and BRD4. As a von Hippel-Lindau (VHL)-based proteolysis-targeting chimera (PROTAC), ARV-771 induces von Hippel-Lindau-dependent polyubiquitination and proteasomal degradation of BET family members. This selective degradation suppresses c-Myc expression and downstream oncogenic signaling pathways, inhibiting cell proliferation and driving apoptosis in castration-resistant prostate cancer models. [1]
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Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
100 mg/mL
(101.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 100 mg/mL |
| Water | Insoluble |
| DMSO |
100 mg/mL
(101.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 100 mg/mL |
| Water | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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