KH-CB19 is a potent CLK (cdc2-like kinase) inhibitor (CLK1 IC50=19.7 nM; CLK3 IC50=530 nM). KH-CB19 shows antiviral activity and inhibits influenza virus replication (IC50=13.6 μM).
| Molecular Weight | 338.19 |
| Formula | C15H13Cl2N3O2 |
| CAS Number | 1354037-26-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 50 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.
[2] Anita Artarini, et al. Antiviral Res. Regulation of influenza A virus mRNA splicing by CLK1
[5] Stephan K Grant, et al. Chem Biol. Kinase inhibition that hinges on halogen bonds
| Related CDK Products |
|---|
| T025
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. |
| PF-07224826
PF-07224826 is a CDK2/4/6 inhibitor. |
| INCB123667
INCB123667 is a CDK2 inhibitor. |
| Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
| Q901
Q901 is a CDK7 inhibitor for tumor-related studies. |
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