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PD-184161

Cat. No. M8046
PD-184161 Structure
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Biological Activity

PD-184161 is a MEK inhibitor.

Chemical Information
Molecular Weight 557.56
Formula C17H13BrClF2IN2O2
CAS Number 212631-67-9
Solubility (25°C) DMSO: ≥10 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] Maroua Jalouli, et al. Selective HIF-1 Regulation under Nonhypoxic Conditions by the p42/p44 MAP Kinase Inhibitor PD184161

[2] Gislaine Z Rus, et al. MAPK signaling correlates with the antidepressant effects of ketamine

[3] Amadeus Gladbach, et al. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke

[4] H Matsushita, et al. Antidepressant-like effect of sildenafil through oxytocin-dependent cyclic AMP response element-binding protein phosphorylation

[5] Jennifer Choi, et al. The effect of doxorubicin on MEK-ERK signaling predicts its efficacy in HCC

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