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CDK12-IN-6
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Catalog No. T40289Cas No. 2651196-71-1
Alias CDK12-IN-6
CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).
CDK12-IN-6
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Catalog No. T40289Alias CDK12-IN-6Cas No. 2651196-71-1
CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 5 mg | $970 | Inquiry | Inquiry |
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Chemical Properties
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| Description | CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1). |
| Targets&IC50 | CDK2-CyclinE:>20 μM (IC50), CDK9-CyclinT1:>20 μM (IC50), CDK12:1.19 μM (IC50) |
| In vitro | CDK12-IN-6 (Example 174) suppresses BRCA1 mRNA expression in MDA-MB-231 cells with an IC50 of 0.872 nM, while having no impact on CAL-120 cells. It also demonstrates antiproliferative effects in both MDA-MB-231 (IC50 = 2.19 nM) and CAL-120 cells (IC50 = 1 nM). Moreover, CDK12-IN-6 exhibits high CDK12 inhibition efficiency with an IC50 to DC50 ratio of 1851, indicating potent activity in hindering CDK12 in ATP to degradation processes. |
| Synonyms | CDK12-IN-6 |
| Molecular Weight | 425.448 |
| Formula | C20H21F2N9 |
| Cas No. | 2651196-71-1 |
| Smiles | Fc1ccc2nc(CNc3nc(nc4c(cnn34)C3CC3)N3CCNCC3)[nH]c2c1F |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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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