الصفحة الرئيسية>>Signaling Pathways>> TGF-β / Smad Signaling>> PKC>>CDK8-IN-12

CDK8-IN-12

رقم الكتالوجGC73183

CDK8-IN-12 هو مثبط CDK8 نشط عن طريق الفم مع Ki من 14 نانومتر.

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CDK8-IN-12 التركيب الكيميائي

Cas No.: 2613307-67-6

الحجم السعر المخزون الكميّة
1 mg
57٫00
متوفر
5 mg
132٫00
متوفر
10 mg
195٫00
متوفر
25 mg
334٫00
متوفر
50 mg
485٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of CDK8-IN-12

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.

Chemical Properties of CDK8-IN-12

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CDK8-IN-12

Prepare stock solution
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
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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