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CDK8/19-IN-51
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Catalog No. T22633Cas No. 1860885-61-5
Alias CCT251545 analogue, Compound 51
CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.
CDK8/19-IN-51
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Purity: 99.62%
Catalog No. T22633Alias CCT251545 analogue, Compound 51Cas No. 1860885-61-5
CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $530 | In Stock | In Stock | |
| 5 mg | $1,170 | In Stock | In Stock | |
| 10 mg | $1,660 | - | In Stock | |
| 25 mg | $2,158 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.62%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers. |
| Targets&IC50 | CDK8:5.1 nM, 7dF3:7.2 nM, p-STAT1727:17.9 nM, CDK19:5.6 nM |
| In vitro | In SW620 human colorectal carcinoma cells harboring an activating APC mutation, CDK8/19-IN-51 inhibited phospho-STAT1^Ser727 with an IC50 of 17.9 nM, which serves as a biomarker of CDK8 inhibition [1]. |
| In vivo | In in vivo pharmacokinetic (PK) studies in mice and rats, CDK8/19-IN-51 exhibited moderate in vivo clearance and volume of distribution (Vd) but showed low bioavailability in mice. In an SW620 human colorectal carcinoma xenograft model, oral administration of CDK8/19-IN-51 (5 mg/kg) inhibited phospho-STAT1^Ser727 in a time-dependent manner. CDK8/19-IN-51 serves as an advanced chemical tool for further investigation of the efficacy, safety, and tolerability of dual CDK8/19 inhibitors [1]. |
| Synonyms | CCT251545 analogue, Compound 51 |
| Molecular Weight | 414.46 |
| Formula | C23H22N6O2 |
| Cas No. | 1860885-61-5 |
| Smiles | O=C(C1=NC2=C(C=NC(N)=C2C=C1)C3=CC=C(C=C3)C=4C=NN(C4)C)N5CC(OC)C5 |
| Relative Density. | no data available |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 8 mg/mL (19.3 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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