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ABD957

Cat. No. M21136
ABD957 Structure
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Quality Control & Documentation
Biological Activity

ABD957 is a potent and selective covalent inhibitor of the ABHD17 family of depalmitoylases, inhibiting IC50 at an IC50 of 0.21 µM. ABD957 impaired N-Ras depalmitylation in AML cells, reducing N-Ras signaling and the growth of NRAS mutant AML cells.

Chemical Information
Molecular Weight 627.68
Formula C27H36F3N7O5S
Solubility (25°C) N/A
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] Jarrett R Remsberg, et al. Nat Chem Biol. ABHD17 regulation of plasma membrane palmitoylation and N-Ras-dependent cancer growth

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