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> ARV-825 [1818885-28-7]

ARV-825 [1818885-28-7]

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Referencia HY-16954-5mg

embalaje : 5mg

Marca : MedChemExpress


Descripciòn

ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

IC50 & Target

Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)[1]
Cellular Effect
Cell Line Type Value Description References
CA46 DC50
<1 nM
Compound: 21; ARV-825
Protac activity at Cereblon/BRD4 in human CA46 cells assessed as induction of BRD4 protein degradation in human CA46 cells after overnight incubation by immunoblot analysis
Protac activity at Cereblon/BRD4 in human CA46 cells assessed as induction of BRD4 protein degradation in human CA46 cells after overnight incubation by immunoblot analysis
[PMID: 31047748]
MOLM-13 IC50
18.2 nM
Compound: 6; ARV-825
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
MOLM-13 IC50
18.2 nM
Compound: ARV-825
Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay
Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay
[PMID: 30019901]
MV4-11 IC50
1.05 nM
Compound: ARV-825
Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay
Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay
[PMID: 30019901]
RS4-11 IC50
3.3 nM
Compound: 6; ARV-825
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
RS4-11 IC50
3.3 nM
Compound: ARV-825
Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay
Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay
[PMID: 30019901]
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 Kds 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ARV-825 Related Antibodies

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 50 mg/mL (54.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureza y Documentación
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