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Lck Inhibitor III

Cat. No. M43529
Lck Inhibitor III Structure
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Biological Activity

Lck Inhibitor III is a potent Lck inhibitor, with an IC50 of 867 nM.

Chemical Information
Molecular Weight 478.54
Formula C25H30N6O4
CAS Number 1188890-30-3
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] Martin Wist et al. J Biol Chem. Noncatalytic Bruton's tyrosine kinase activates PLCγ2 variants mediating ibrutinib resistance in human chronic lymphocytic leukemia cells

[2] Lucie Cornet et al. Eur Respir J. Pulmonary arterial hypertension associated with protein kinase inhibitors: a pharmacovigilance-pharmacodynamic study

[3] Markus Lindauer et al. Recent Results Cancer Res. Dasatinib

[4] B D Kahan. Transplant Proc. Frontiers in immunosuppression

[5] Markus Lindauer et al. Recent Results Cancer Res. Dasatinib

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