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CC-90005

Cat. No. M21183
CC-90005  Structure
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Quality Control & Documentation
Biological Activity

CC-90005 is a potent, selective and orally active protein kinase C-θ (PKC-θ) inhibitor with an IC50 value of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation via IL-2 expression.

Chemical Information
Molecular Weight 447.48
Formula C21H27F2N7O2
CAS Number 1799574-70-1
Solubility (25°C) DMSO : 62.5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Patrick Papa, et al. J Med Chem. Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005

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