| Molecular Formula | C18H18ClN5O |
| Molar Mass | 355.82 |
| Density | 1.356 |
| Melting Point | 144-147℃ |
| Boling Point | 630.6±65.0 °C(Predicted) |
| pKa | 14.93±0.10(Predicted) |
| Storage Condition | 2-8°C(protect from light) |
| In vitro study | CGP60474 (Compound A) is a potent VEGFR-2 inhibitor, with an IC 50 of 84 nM. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP. |
| In vivo study | CGP-60474 (10 mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate in the LPS endotoxemia model. Animal Model: C57Bl/6 mice (LPS endotoxemia model) Dosage: 10 mg/kg Administration: I.p. Result: Had a higher survival rate. |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.81 ml | 14.052 ml | 28.104 ml |
| 5 mM | 0.562 ml | 2.81 ml | 5.621 ml |
| 10 mM | 0.281 ml | 1.405 ml | 2.81 ml |
| 5 mM | 0.056 ml | 0.281 ml | 0.562 ml |
| biological activity | CGP60474 is an efficient anti-endotoxin drug, it is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values for 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. |
| target | CDK1-Cyclin B 26 nM (IC 50 ) CDK2/cyclinE 3 nM (IC 50 ) cdk2/cyclin A 4 nM (IC 50 ) CDK4/cyclin D 216 nM (IC 50) Cdk5/P25 10 nM (IC 50 ) CDK7/cyclin H 200 nM (IC 50 ) CDK9/cycT 13 nM (IC 50 ) PKC |
| in vitro study | CGP60474 (Compound a) is a potent VEGFR-2 inhibitor, with an IC 50 of 84 nM. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP. |
| in vivo study | CGP-60474 (10 mg/kg; I.p.) inhibits the IL-6 level and increases the survival rate in the LPS endotoxemia model. Animal Model: C57Bl/6 MICE (LPS endotoxemia model) Dosage: 10 mg/kg Administration: I.p. Result: had a higher survival rate. |
| Animal Model: | C57Bl/6 mice (LPS endotoxemia model) |
| Dosage: | 10 mg/kg |
| Administration: | I .p. |
| Result: | Had a higher survival rate. |