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CDK12-IN-4
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Catalog No. T40288Cas No. 2651196-69-7
Alias CDK12-IN-4
CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).
CDK12-IN-4
😃Good
Catalog No. T40288Alias CDK12-IN-4Cas No. 2651196-69-7
CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $970 | Inquiry | Inquiry |
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| Description | CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1). |
| Targets&IC50 | CDK2-CyclinE:>20 μM (IC50), CDK12:0.641 μM (IC50), CDK9-CyclinT1:>20 μM (IC50) |
| In vitro | CDK12-IN-4 (Example 172) selectively inhibits BRCA1 mRNA expression in MDA-MB-231 cells with an IC50 value of 0.626 nM, without affecting CAL-120 cells. It demonstrates antiproliferative effects in MDA-MB-231 and CAL-120 cells, with IC50 values of 0.535 nM and 2.43 nM, respectively, and a high CDK12 inhibition potency with an IC50 to degradation DC50 ratio of 581, indicating effectiveness and selective action [1]. |
| Synonyms | CDK12-IN-4 |
| Molecular Weight | 426.432 |
| Formula | C20H20F2N8O |
| Cas No. | 2651196-69-7 |
| Smiles | Fc1ccc2nc(CNc3nc(nc4c(cnn34)C3CC3)N3CCOCC3)[nH]c2c1F |
| 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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