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CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $168 | In Stock | In Stock | |
| 5 mg | $419 | In Stock | In Stock | |
| 10 mg | $679 | In Stock | In Stock | |
| 25 mg | $1,390 | In Stock | In Stock | |
| 50 mg | $2,190 | In Stock | In Stock | |
| 100 mg | $2,970 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $463 | In Stock | In Stock |
| Description | CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer. |
| Targets&IC50 | CDK12:23.9 nM, CDK9-cyclinT1:127 μM, CDK2-CyclinE:173 μM |
| In vitro | CDK12-IN-5 (Example 426) selectively suppresses BRCA1 mRNA levels in MDA-MB-231 cells (IC50 = 3.23 nM) without affecting CAL-120 cells. It exhibits antiproliferative effects on both MDA-MB-231 (IC50 = 4.19 nM) and CAL-120 cells (IC50 = 3.57 nM). Additionally, CDK12-IN-5 demonstrates high selectivity for CDK12 inhibition with an IC50 to DC50 CDK12 ratio of 32[1]. |
| Molecular Weight | 454.36 |
| Formula | C18H15F5N8O |
| Cas No. | 2651200-35-8 |
| Smiles | FC=1C=CC=2N=C(NC2C1F)CNC3=NC(=NC4=C(C=NN34)C(F)(F)F)N5CCOCC5 |
| Relative Density. | 1.77 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (220.09 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (7.26 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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.
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.
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