CGP60474 is a highly effective anti-endotoxin drug, It is an effective cyclin-dependent kinase (CDK) inhibitor (IC50 of CDK1/B, CDK2/E, CDK2/ A, CDK4/D, CDK5/ P25, CDK7/H and CDK9/T are 26, 3, 4, 216, 10, 200 and 13 nM, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
| Molecular Weight | 355.82 |
| Formula | C18H18ClN5O |
| CAS Number | 164658-13-3 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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Vanicoside B targets cyclin-dependent kinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis. |
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