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 modelIn VitroPERK-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 VivoPERK-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:SolidIC50& Target:IC 50 : 2 nM (PERK), 9 nM (p-eIF2α). Specification: 0.99 Molecular Formula: C25H26F2N4O3 Molecular Weight: 468.5
- UPC:
- 51171652
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- P649188-5mg
- CAS:
- 2616821-91-9
- Product Size:
- 5mg
