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CAN508 is a potent ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Antitumor activity.]

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $30 | In Stock | In Stock | |
| 10 mg | $41 | In Stock | In Stock | |
| 25 mg | $88 | In Stock | In Stock | |
| 50 mg | $133 | In Stock | In Stock | |
| 100 mg | $198 | In Stock | In Stock | |
| 200 mg | $291 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $34 | In Stock | In Stock |
| Description | CAN508 is a potent ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Antitumor activity.] |
| Targets&IC50 | CDK1-CyclinB:44 μM, CDK9-CyclinT1:0.35 μM, Cdk4-CyclinD1:13.5 μM, CDK2-CyclinE:20 μM, CDK2-CyclinA:69 μM, CDK7-CyclinH:26 μM |
| In vitro | The most potent inhibitor,CAN508, reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.?Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9. |
| Molecular Weight | 218.22 |
| Formula | C9H10N6O |
| Cas No. | 140651-18-9 |
| Smiles | Nc1n[nH]c(N)c1\N=N\c1ccc(O)cc1 |
| Relative Density. | 1.67 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (1145.63 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (22.91 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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