GS-626510
Based on 1 Customer Validation
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively.
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 1637770-13-8
- Formula: C25H22N4O
- Molecular Weight:394.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD2 0.59-2.5 nM (Kd) |
BRD3 0.65-0.66 nM (Kd) |
BRD4 1.3-3.2 nM (Kd) |
BD1 83 nM (IC50) |
BD2 78 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | EC50 |
58 nM
Compound: 42
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Antiproliferative activity against human MM1S cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MM1S cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 30606676] |
| MT4 | EC50 |
18 nM
Compound: 42
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
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[PMID: 30606676] |
| SU-DHL10 | EC50 |
31 nM
Compound: 42
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Antiproliferative activity against human SU-DHL10 cells
Antiproliferative activity against human SU-DHL10 cells
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[PMID: 30606676] |
Chemical Information
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CAS No. 1637770-13-8
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Appearance Solid
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Molecular Weight 394.47
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Formula C25H22N4O
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Color White to off-white
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SMILES
CC1=C(C2=CC(C3=C4C=CC=NC4=CC=C3C)=C5NC(C6CC6)=NC5=C2)C(C)=NO1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (63.38 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.34 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.34 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL | 63.3762 mL |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL | 12.6752 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 6.3376 mL | |
| 15 mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 4.2251 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2675 mL | 3.1688 mL | |
| 25 mM | 0.1014 mL | 0.5070 mL | 1.0140 mL | 2.5350 mL | |
| 30 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1125 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5844 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4225 mL | 1.0563 mL |
GS-626510 Related Classifications
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