(Rac)-BRD0705
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
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- CAS No.: 1597440-03-3
- 화학식: C20H23N3O
- 분자량:321.42
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
Chemical Information
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CAS No. 1597440-03-3
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Appearance Solid
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분자량 321.42
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화학식 C20H23N3O
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Color Light yellow to yellow
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SMILES
O=C1C2=C(N=C3C(C2(CC)C4=CC=CC=C4)=CNN3)CC(C)(C)C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 250 mg/mL (777.80 mM; Need ultrasonic; 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: ≥ 2.08 mg/mL (6.47 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 (6.47 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.
순도&문서
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Data Sheet (278 KB)
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SDS (102 KB)
- English - EN (102 KB)
- Français - FR (102 KB)
- Deutsch - DE (102 KB)
- Norwegian - NO (102 KB)
- Español - ES (102 KB)
- Swedish - SV (102 KB)
- Italian - IT (102 KB)
- Korean - KR (102 KB)
- Portuguese - PT (102 KB)
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Handling Instructions (2659 KB)
References
[1]. Wagner FF, et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. [Content Brief]
[2]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1.
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 | 3.1112 mL | 15.5560 mL | 31.1119 mL | 77.7798 mL |
| 5 mM | 0.6222 mL | 3.1112 mL | 6.2224 mL | 15.5560 mL | |
| 10 mM | 0.3111 mL | 1.5556 mL | 3.1112 mL | 7.7780 mL | |
| 15 mM | 0.2074 mL | 1.0371 mL | 2.0741 mL | 5.1853 mL | |
| 20 mM | 0.1556 mL | 0.7778 mL | 1.5556 mL | 3.8890 mL | |
| 25 mM | 0.1244 mL | 0.6222 mL | 1.2445 mL | 3.1112 mL | |
| 30 mM | 0.1037 mL | 0.5185 mL | 1.0371 mL | 2.5927 mL | |
| 40 mM | 0.0778 mL | 0.3889 mL | 0.7778 mL | 1.9445 mL | |
| 50 mM | 0.0622 mL | 0.3111 mL | 0.6222 mL | 1.5556 mL | |
| 60 mM | 0.0519 mL | 0.2593 mL | 0.5185 mL | 1.2963 mL | |
| 80 mM | 0.0389 mL | 0.1944 mL | 0.3889 mL | 0.9722 mL | |
| 100 mM | 0.0311 mL | 0.1556 mL | 0.3111 mL | 0.7778 mL |
(Rac)-BRD0705 Related Classifications
HY-116830A Related Classifications
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