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PF-6260933

Cat. No. M20578
PF-6260933 Structure
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Biological Activity

PF-6260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity.

Chemical Information
Molecular Weight 296.75
Formula C16H13ClN4
CAS Number 1811510-56-1
Solubility (25°C) DMSO 59 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] Jin Yang, et al. Biomed Pharmacother. Intestinal epithelial cell-derived exosomes package microRNA-23a-3p alleviate gut damage after ischemia/reperfusion via targeting MAP4K4

[2] Gi Suk Nam, et al. Biochem Pharmacol. A new function for MAP4K4 inhibitors during platelet aggregation and platelet-mediated clot retraction

[3] Rachel J Roth Flach, et al. Nat Commun. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis

[4] Mark Ammirati, et al. ACS Med Chem Lett. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment

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Keywords: PF-6260933 supplier, Serine/Threonine Protease, inhibitors, activators

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