PERK-IN-5 是一种高效、高选择性且口服生物可利用的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂，PERK 与 p-eIF2α 的 IC50 为 2 nM 和 9 nM。PERK-IN-5 在 786-O 肾细胞癌异种移植瘤模型中，能显著抑制肿瘤生长。
货号:ajcx38450
CAS:2616821-91-9
分子式:C25H26F2N4O3
分子量：468.5
溶解度:DMSO : 250 mg/mL (533.62 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.