GNE-064
Based on 1 Customer Validation
GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis.
For research use only. We do not sell to patients.
- Purity: 99.65%
- CAS No.: 1997321-20-6
- Formula: C17H21N5O2
- Molecular Weight:327.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Biological Activity
IC50: 0.035 μM (SMARCA4)[1]
GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ZsGreen-SMARCA2 BD-expressing U2OS cells
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Concentration:0-0.5 μM
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Incubation Time:1 hour
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Result:Inhibited SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells with an EC50 of 0.1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD-1 mice[1]
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Dosage:0.5 mg/kg (i.v.) and 1.0 mg/kg (p.o.)
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Administration:Intravenous injection and oral gavage; 0.5 mg/kg and 1.0 mg/kg once
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Result:Showed a low unbound plasma clearance with 16 mL/min/kg, a reasonable half-life of 1.1 h and good oral bioavailability of 59%.
Chemical Information
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CAS No. 1997321-20-6
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Appearance Solid
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Molecular Weight 327.38
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Formula C17H21N5O2
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Color Light yellow to yellow
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SMILES
CC(N1[C@H](C)CN(C2=CC(C3=CC=CC=C3O)=NN=C2N)CC1)=O
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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 : ≥ 125 mg/mL (381.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.08 mg/mL (6.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (286 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 3.0546 mL | 15.2728 mL | 30.5455 mL | 76.3639 mL |
| 5 mM | 0.6109 mL | 3.0546 mL | 6.1091 mL | 15.2728 mL | |
| 10 mM | 0.3055 mL | 1.5273 mL | 3.0546 mL | 7.6364 mL | |
| 15 mM | 0.2036 mL | 1.0182 mL | 2.0364 mL | 5.0909 mL | |
| 20 mM | 0.1527 mL | 0.7636 mL | 1.5273 mL | 3.8182 mL | |
| 25 mM | 0.1222 mL | 0.6109 mL | 1.2218 mL | 3.0546 mL | |
| 30 mM | 0.1018 mL | 0.5091 mL | 1.0182 mL | 2.5455 mL | |
| 40 mM | 0.0764 mL | 0.3818 mL | 0.7636 mL | 1.9091 mL | |
| 50 mM | 0.0611 mL | 0.3055 mL | 0.6109 mL | 1.5273 mL | |
| 60 mM | 0.0509 mL | 0.2545 mL | 0.5091 mL | 1.2727 mL | |
| 80 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9545 mL | |
| 100 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7636 mL |
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