PERK-IN-5

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor ( IC 50 s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model In Vitro PERK-IN-5 (compound 28) (10-48 µM) is relatively stable in both human and dog hepatocytes and is characterized with long half-lives. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PERK-IN-5 (3-100 mg/kg; p.o.; 0.25-24 hours) has robust pharmacokinetics in CD1 mice, with C max of 3353 ng/mL, AUC 0-last of 5153 h*ng/mL, and bioavailability of 70% . PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD1 mice (Pharmacokinetics) Dosage: 3, 10, 30 and 100 mg/kg Administration: p.o.; 0.25-24 hours Result: Showed robust pharmacokinetics with C max of 3353 ng/mL, AUC 0-last of 5153 h*ng/mL, and bioavailability of 70%. Animal Model: BALB/c nude female mice (inoculated subcutaneously with 786-O tumor cells) Dosage: 3 or 10 mg/kg Administration: p.o.; twice daily, for 28 days Result: Showed statistically significant tumor growth inhibition. Form:Solid IC50& Target:IC 50 : 2 nM (PERK), 9 nM (p-eIF2α)

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