PERK-IN-5 |
| رقم الكتالوجGC64866 |
PERK-IN-5 هو مثبط PERK قوي للغاية وانتقائي ومتوفر بيولوجيًا عن طريق الفم (IC50s من 2 و 9 نانومتر لـ PERK و p-eIF2α ، على التوالي)يمكن أن يمنع PERK-IN-5 نمو الورم بشكل كبير في نموذج ورم سرطان الخلايا الكلوية 786-O
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2616821-91-9
Sample solution is provided at 25 µL, 10mM.
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PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s 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[1].
PERK-IN-5 (compound 28) (10-48 µM) is relatively stable in both human and dog hepatocytes and is characterized with long half-lives[1].
PERK-IN-5 (3-100 mg/kg; p.o.; 0.25-24 hours) has robust pharmacokinetics in CD1 mice, with Cmax of 3353 ng/mL, AUC0-last of 5153 h*ng/mL, and bioavailability of 70%[1].PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition[1].
[1]. Calvo V, et al. Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors. Bioorg Med Chem Lett. 2021;43:128058.
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