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ETP-46321

Cat. No. M22279
ETP-46321 Structure
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Biological Activity

ETP-46321

Chemical Information
Molecular Weight 473.55
Formula C20H27N9O3S
CAS Number 1252594-99-2
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] Sonia Martnez Gonzlez, et al. Bioorg Med Chem Lett. Identification of novel PI3K inhibitors through a scaffold hopping strategy

[2] Sonia Martnez Gonzlez, et al. Bioorg Med Chem Lett. Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy

[3] L Aragoneses-Fenoll, et al. Biochem Pharmacol. ETP-46321, a dual p110α/δ class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis

[4] Teresa G Granda, et al. Invest New Drugs. Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases

[5] Sonia Martnez Gonzlez, et al. Bioorg Med Chem Lett. Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor

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