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GNE-9815

Cat. No. M21135
GNE-9815 Structure
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Biological Activity

GNE-9815 is one of the most selective kinase inhibitors of RAF, targeting KRAS mutant cancers by combination of drugs.

Chemical Information
Molecular Weight 455.48
Formula C26H22FN5O2
CAS Number 2729996-45-4
Solubility (25°C) DMSO : 50 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] Malcolm P Huestis, et al. ACS Med Chem Lett. Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor

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  Catalog
Abmole Inhibitor Catalog




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