产品
编 号：F754072
分子式：C25H26F2N4O3
分子量：468.5
分子式：C25H26F2N4O3
分子量：468.5
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2616821-91-9
产品详情
生物活性：
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.
体内研究：
PERK-IN-5 (3-100 mg/kg；口服；0.25-24 小时) 在 CD1 小鼠中具有稳健的药代动力学，Cmax 为 3353 ng/mL，AUC0-last为 5153 h*ng/mL，生物利用度为 70%。 PERK-IN-5 (3 或 10 mg/kg；口服；每天两次，28 天) 具有显著的肿瘤生长抑制作用。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 Cmax of 3353 ng/mL, AUC0-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.
体外研究：
PERK-IN-5 (化合物 28) (10-48 μM) 在人和狗的肝细胞中都相对稳定，具有较长的半衰期。
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.
体内研究：
PERK-IN-5 (3-100 mg/kg；口服；0.25-24 小时) 在 CD1 小鼠中具有稳健的药代动力学，Cmax 为 3353 ng/mL，AUC0-last为 5153 h*ng/mL，生物利用度为 70%。 PERK-IN-5 (3 或 10 mg/kg；口服；每天两次，28 天) 具有显著的肿瘤生长抑制作用。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 Cmax of 3353 ng/mL, AUC0-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.
体外研究：
PERK-IN-5 (化合物 28) (10-48 μM) 在人和狗的肝细胞中都相对稳定，具有较长的半衰期。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备