PERK-IN-5

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PERK-IN-5

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2616821-91-9

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议

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 bioavailablePERKinhibitor (IC₅₀s of 2 and 9 nM forPERKand p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model^[1].

IC₅₀& Target

IC₅₀: 2 nM (PERK), 9 nM (p-eIF2α)^[1]

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

PERK-IN-5 (3-100 mg/kg; p.o.; 0.25-24 hours) has robust pharmacokinetics in CD1 mice, with C_maxof 3353 ng/mL, AUC_0-lastof 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_maxof 3353 ng/mL, AUC_0-lastof 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.

分子量

468.50

性状

Solid

Formula

C₂₅H₂₆F₂N₄O₃

CAS 号

2616821-91-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。