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CAS No.: 1337531-36-8

GSK2606414 Catalog No. CSN15902

Synonyms: GSK PERK Inhibitor

GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PERK

IC50:0.4nM
描述UPR (unfolded protein response), dysregulation of which has been implicated in many important pathologies, is an essential pathway to cope with ER stress. PERK is one of three primary effectors of the UPR. It can be activated by the released ER chaperones caused by increase of unfolded proteins in the ER and thus phosphorylates eIF2α. GSK2606414 is a potent and selective PERK inhibitor with IC50 value of 0.4nM (measured by cytoplasmic PERK domain phosphorylation of EIF2α). Treatment with GSK2606414 at concentration ranging in 0.03-0.3μM for 2h can significantly inhibit p-PERK induced by 1μM thapsigargin with IC50 value<0.03μM in A549 cells. Oral administration of GSK2606414 at dose of 50mg/kg and 150mg/kg, b.i.d., for 21 days showed antitumor activity in a human pancreatic tumor xenograft model^[1].
作用机制The trifluoromethyl meta-substituent of GSK2606414 can occupy the PERK kinase domain.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A549 cells	-	Function assay	2 h	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting	22827572
human A549 cells	0.03 μM	Function assay	2 h	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells at 0.03 uM after 2 hrs by Western blotting	22827572
human A549 cells	-	Function assay	1 h	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis	24900593

动物研究

剂量

Mice: 0.25 mg/kg - 5 mg/kg^[2] (i.p.); 50 mg/kg - 150 mg/kg^[3] (p.o.)

给药途径

i.p., p.o.

动物药代数据

Animal	Mice^[1]	Rats^[1]	Dogs^[1]
Dose	1.7 mg/kg	2.1 mg/kg	2.7 mg/kg
Administration	i.v.	i.v.	i.v.
CL_b	31.8 ml/min/kg	21.5 ml/min/kg	12.5 ml/min/kg
T_1/2	2.5 h	2.5 h	10.6 h
Vd_ss	5.1 L/kg	3.8 L/kg	8.2 L/kg
AUC_0→t	839.1 ng·h/ml	1602.1 ng·h/ml	3155.3 ng·h/ml

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2151 mL
- 11.0756 mL
- 22.1512 mL
- 5 mM
- 0.4430 mL
- 2.2151 mL
- 4.4302 mL
- 10 mM
- 0.2215 mL
- 1.1076 mL
- 2.2151 mL

技术信息

CAS号

1337531-36-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H20F3N5O

运输

蓝冰

分子量

451.44

别名

GSK PERK Inhibitor

溶解度

DMSO	500.0 mg/mL (1107.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	31 mg/mL	suspension

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