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。

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 [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 C max of 3353 ng/mL, AUC 0-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]. Animal Model: Female CD1 mice [1] (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) [1] Dosage: 3 or 10 mg/kg Administration: p.o.; twice daily, for 28 days Result: Showed statistically significant tumor growth inhibition.

2616821-91-9

C25H26F2N4O3

468.5

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years