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Trametiglue

Cat. No. M42141
Trametiglue Structure
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Biological Activity

Trametiglue, a derivative of Trametinib, targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions.

Chemical Information
Molecular Weight 666.46
Formula C25H24FIN6O5S
CAS Number 2666940-97-0
Form Solid
Solubility (25°C) DMSO 90 mg/mL (ultrasonic and warming)
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] Zaigham M Khan et al. Nature. Structural basis for the action of the drug trametinib at KSR-bound MEK

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Keywords: Trametiglue supplier, MEK, inhibitors, activators


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