CDK8-IN-12 |
رقم الكتالوجGC73183 |
CDK8-IN-12 هو مثبط CDK8 نشط عن طريق الفم مع Ki من 14 نانومتر.
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Cas No.: 2613307-67-6
Sample solution is provided at 25 µL, 10mM.
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent.
CDK8-IN-12 (compound 38) selectively inhibits the proliferation of MV4-11 acute myeloid leukaemia cells with a GI50 of 0.36 μM[1]. CDK8-IN-12 (0.36, 0.72 μM; 2 hours) significantly reduces the phosphorylation of serine 727 on STAT1[1].
CDK8-IN-12 (compound 38; IV; 5 mg/kg for rat and 2 mg/kg for mouse) has a T1/2 of 0.9 hours and 0.34 hours for rat and mouse, respectively[1]. Pharmacokinetic Parameters of CDK8-IN-12 [1].
References:
[1]. Mingfeng Yu, et al. Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. Eur J Med Chem. 2021 Mar 15;214:113248.
Cas No. | 2613307-67-6 | SDF | |
Formula | C21H20ClN3O2 | M.Wt | 381.86 |
الذوبان | DMSO : 66.67 mg/mL (174.59 mM; Need ultrasonic) | Storage | -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 | 2.6188 mL | 13.0938 mL | 26.1876 mL |
5 mM | 0.5238 mL | 2.6188 mL | 5.2375 mL |
10 mM | 0.2619 mL | 1.3094 mL | 2.6188 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >99.00%
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