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.
|Solubility (25°C)||DMSO ≥ 40 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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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JH-VIII-49 is a potent, highly selective CDK8 inhibitor with a simple steroidal core.
Cortistatin A is a potent, selective inhibitor of CDK8 and CDK19.
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.
FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader.
CK7 is a Cdk2/9 inhibitor, which can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.
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