[CAS NO. 1818885-28-7] ARV-825
PRODUCTS SPECIFICATIONS [1818885-28-7]
DESCRIPTION [1818885-28-7]
Overview
| MDL | MFCD29472237 |
|---|---|
| Molecular Weight | 923.43 |
| Molecular Formula | C46H47ClN8O9S |
| SMILES | CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O |
13 Publications Citing Use of MCE
- [1]Nat Commun. 2022 Jul 18;13(1):4157.
- [2]Nat Commun. 2022 Jan 10;13(1):183.
- [3]Nat Commun. 2020 Aug 14;11(1):4083.
- [4]Nat Commun. 2020 Apr 22;11(1):1935.
- [5]Clin Cancer Res. 2019 Jun 1;25(11):3404-3416.
- [6]JCI Insight. 2022 May 9;7(9):e150871.
- [7]Aging. 2020 Mar 12;12(5):4547-4557.
- [8]Hum Gene Ther. 2022 Nov 14.
- [9]J Biol Chem. 2022 Mar 3;101794.
- [10]Sci Rep. 2018 Sep 5;8(1):13225.
- [11]Research Square Print. November 18th, 2022
- [12]Nature Aging. 25 January 2022.
- [13]Martin-Luther-Universität Halle-Wittenberg. Naturwissenschaftlichen Fakultät I. 2020 Dec.
Summary
IC50 & Target
Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4) [1]
In Vitro
ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have K d s of 28-90 nM and ~3 µM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 54.15 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.0829 mL | 5.4146 mL | 10.8292 mL |
| 5 mM | 0.2166 mL | 1.0829 mL | 2.1658 mL |
| 10 mM | 0.1083 mL | 0.5415 mL | 1.0829 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution