(Rac)-BRD0705 |
カタログ番号GC39058
One-Click Copy Product Info
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(Rac)-BRD0705 は、BRD0705 の活性の低いラセミ体です。 BRD0705 は、66 nM の IC50 と 4.8 μM の Kd を持つ強力なパラログ選択的経口活性 GSK3α 阻害剤です。 BRD0705 は、GSK3β (515 nM の IC50) に対して GSK3α (8 倍) に対する選択性の増加を示します。 BRD0705 は、急性骨髄性白血病 (AML) に使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1597440-03-3
Sample solution is provided at 25 µL, 10mM.
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(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 to treat acute myeloid leukemia (AML)[1][2].
[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. [2]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1.
| Cas No. | 1597440-03-3 | SDF | |
| Canonical SMILES | O=C1C2=C(N=C3C(C2(CC)C4=CC=CC=C4)=CNN3)CC(C)(C)C1 | ||
| Formula | C20H23N3O | M.Wt | 321.42 |
| 溶解度 | DMSO: 250 mg/mL (777.80 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1112 mL | 15.556 mL | 31.1119 mL |
| 5 mM | 622.2 μL | 3.1112 mL | 6.2224 mL |
| 10 mM | 311.1 μL | 1.5556 mL | 3.1112 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)