CDK9-IN-7 |
| カタログ番号GC35636 |
CDK9-IN-7 (化合物 21e) は、選択的で非常に強力な経口活性 CDK9/サイクリン T 阻害剤 (IC50=11 nM) であり、他の CDK (CDK4/cyclinD=148 nM; CDK6/cyclinD= 145 nM)。 CDK9-IN-7 は明らかな毒性のない抗腫瘍活性を示します。 CDK9-IN-7 は、NSCLC 細胞のアポトーシスを誘導し、G2 期の細胞周期を停止させ、NSCLC の幹細胞性を抑制します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2369981-71-3
Sample solution is provided at 25 µL, 10mM.
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CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC[1]. CDK9/cyclinT1|11 nM (IC50)|CDK4/cyclin D|148 nM (IC50)|CDK6/cyclinD|145 nM (IC50)
CDK9-IN-7 displays exceptional potency against NSCLC cell lines, especial A549 and H1299 with IC50 values less than 0.5 µM. In the drug-resistant NSCLC cell line H1975, CDK9-IN-7 also exhibits good inhibition potency with an IC50 value of 0.837 µM[1].
[1]. Wang X, et al. Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer. Eur J Med Chem. 2019 Jul 25;181:111535.
| Cas No. | 2369981-71-3 | SDF | |
| Canonical SMILES | O=C(N(C)C)C1=CC2=CN=C(NC3=CC=C(NC(CCCCCCCN=C=S)=O)C=C3)N=C2N1C4CCCC4 | ||
| Formula | C29H37N7O2S | M.Wt | 547.71 |
| 溶解度 | DMSO: 62.5 mg/mL (114.11 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8258 mL | 9.1289 mL | 18.2578 mL |
| 5 mM | 0.3652 mL | 1.8258 mL | 3.6516 mL |
| 10 mM | 0.1826 mL | 0.9129 mL | 1.8258 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 ddH2O, 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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