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CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $132 | - | In Stock | |
| 5 mg | $328 | - | In Stock | |
| 10 mg | $496 | - | In Stock | |
| 25 mg | $873 | - | In Stock | |
| 50 mg | $1,180 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $363 | - | In Stock |
| Description | CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer. |
| Targets&IC50 | CDK2-CyclinA:932 nM, CDK7-CyclinH-MNAT1:1210 nM, CDK9-CyclinT1:23.9 nM |
| In vitro | CDK12-IN-E9 treatment of Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82, and NCI-H3122 cells after 72 hours of action in the concentration range of 10 nM to 10 μM showed significant antiproliferative activity against THZ1R neuroblastoma and lung cancer cells, with IC50 values ranging from 8 to 40 nM. After 6 hours of action in the concentration range of 0 to 3000 nM, CDK12-IN-E9 treatment of Kelly, PC-9, and NCI-H82 cells induced a dose-dependent decrease in phosphorylated and total RNAPII accompanied by a decrease in MYC and MCL1 expression in THZ1R neuroblastoma and lung cancer models. In addition, CDK12-IN-E9 increased PARP cleavage and elevated the proportion of sub-G1 phase cells in THZ1R lung cancer cells, whereas it was more likely to cause G2/M phase block in neuroblastoma cells after 24 hours of exposure. [1] |
| Molecular Weight | 434.53 |
| Formula | C24H30N6O2 |
| Cas No. | 2020052-55-3 |
| Smiles | C(C)C1=C2N(C(NC3=CC(NC(C=C)=O)=CC=C3)=CC(=N2)N4[C@H](CCO)CCCC4)N=C1 |
| Relative Density. | 1.28 g/cm3 (Predicted) |
| Color | Yellow |
| Appearance | Solid |
| 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 (230.13 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.21 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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