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PD 198306

Cat. No. M2915
PD 198306 Structure
Size Price Availability
10mg USD 170  USD170 Custom Synthesis
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Quality Control & Documentation
Biological Activity

PD 198306 is a cell-permeable and highly selective MEK inhibitor with IC50 of 8 nM.

Chemical Information
Molecular Weight 476.23
Formula C18H16F3IN2O2
CAS Number 212631-61-3
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Benoit Besson, et al. Kinome-Wide RNA Interference Screening Identifies Mitogen-Activated Protein Kinases and Phosphatidylinositol Metabolism as Key Factors for Rabies Virus Infection

[2] Jade M Franklin, et al. Cannabinoid receptor agonists upregulate and enhance serotonin 2A (5-HT(2A)) receptor activity via ERK1/2 signaling

[3] Edita Aksamitiene, et al. PI3K/Akt-sensitive MEK-independent compensatory circuit of ERK activation in ER-positive PI3K-mutant T47D breast cancer cells

[4] Jean-Pierre Pelletier, et al. In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes

[5] A Ciruela, et al. Identification of MEK1 as a novel target for the treatment of neuropathic pain

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  Catalog
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Keywords: PD 198306 supplier, MEK, inhibitors, activators


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