PERK-IN-5|cas:2616821-91-9|西域试剂

PERK-IN-5,99.40%

产品编号：Bellancom-145835| CAS NO：2616821-91-9| 分子式：C₂₅H₂₆F₂N₄O₃| 分子量：468.50

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-145835		￥7500.00	杭州北京（现货）
Bellancom-145835		￥12000.00	杭州北京（现货）

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PERK-IN-5

产品介绍

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。

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.

体外研究

PERK-IN-5 (compound 28) (10-48 µM) is relatively stable in both human and dog hepatocytes and is characterized with long half-lives.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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%.
PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition.

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (533.62 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1345 mL	10.6724 mL	21.3447 mL
5 mM	0.4269 mL	2.1345 mL	4.2689 mL
10 mM	0.2134 mL	1.0672 mL	2.1345 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式