CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells. It has pan-PKD inhibitory effects (PKD2 IC50 = 0.6±0.1; PKD3 IC50 = 0.7±0.2 uM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor.Protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). Cell permeable (EC50 = 10 μM for PKD1 inhibition).
Molecular Weight | 396.87 |
Formula | C22H21ClN2O3 |
CAS Number | 638156-11-3 |
Solubility (25°C) | DMSO |
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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