7-甲基-5-[1-[[3-(三氟甲基)苯基]乙酰基]-2,3-二氢-1H-吲哚-5-基]-7H-吡咯并[2,3-d]嘧啶-4-胺

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E-苯乙烯硼酸频那醇酯
4-bromo-5-chloro-2-methylpyridine
1,3-双[2-(4-氨基苯基)-2-丙基]苯
甘草酚
丙磺舒
考布他丁 A-4 磷酸二钠盐

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中文名	7-甲基-5-[1-[[3-(三氟甲基)苯基]乙酰基]-2,3-二氢-1H-吲哚-5-基]-7H-吡咯并[2,3-d]嘧啶-4-胺
英文名	1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone
英文别名	更多

描述

GSK2606414是可渗透细胞且可口服的 PERK 抑制剂，IC50值为0.4 nM。

相关类别

信号通路 >>

细胞周期/DNA损伤 >>

PERK

研究领域 >>

癌症

靶点

EIF2AK3 (PERK):0.4 nM (IC50)

EIF2AK1 (HRI):420 nM (IC50)

EIF2AK2 (PKR):696 nM (IC50)

体外研究

GSK2606414抑制细胞中PERK的活化[1]。

体内研究

GSK2606414（50和150mg / kg，po）抑制小鼠中人肿瘤异种移植物的生长[1]。

溶解度

体外：

DMSO：≥31mg / mL（68.67 mM）

* “≥”表示可溶，但饱和度未知。

体内：1.GSK2606414在含有0.5％羟丙基甲基纤维素和0.1％吐温80的溶液中制备[2]。

储备液

1 mM	2.2151 mL	11.0757 mL	22.1513 mL
5 mM	0.4430 mL	2.2151 mL	4.4303 mL
10 mM	0.2215 mL	1.1076 mL	2.2151 mL

动物实验

将来自细胞培养物的指数生长的BxPC3肿瘤细胞（10×10 6个细胞/小鼠）皮下植入雌性裸鼠的右胁腹。植入后16天，将具有-200mm 3肿瘤的小鼠随机分成各种治疗组（n = 8只小鼠/组）。用载体（0.5％羟丙基甲基纤维素，0.1％吐温80水溶液，pH4.8），化合物50或150mg / kg口服处理动物，投标21天。用卡尺每周测量肿瘤体积两次并计算。结果表示为给药完成时的抑制百分比，其为100 [1-（药物处理群体的平均生长）/（载体处理的对照群体的平均生长）]。使用双尾t检验进行统计分析。

存储

粉末	-20°C	3年
?	4°C	2年
在溶剂中	-80°C	6月
?	-20°C	1月

运输

室温;可能会有所不同

SMILES

NC1=C2C(N(C)C=C2C3=CC4=C(N(C(CC5=CC=CC(C(F)(F)F)=C5)=O)CC4)C=C3)=NC=N1

参考文献

[1]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulu

[2]. Zhang M, et al. Inhibiting the Plasmodium eIF2α Kinase PK4 Prevents Artemisinin-Induced Latency. Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.

相关活性
小分子

5-[4-氟-1-[(6-甲基-2-吡啶基)乙酰基]-2,3-二氢-1H-吲哚-5-基]-7-甲基-7H-吡咯并[2,3-d]嘧啶-4-胺

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ISRIB(反式异构体)

|

CCT020312

密度	1.4±0.1 g/cm3
沸点	720.3±60.0 °C at 760 mmHg
分子式	C₂₄H₂₀F₃N₅O
分子量	451.444
闪点	389.4±32.9 °C
精确质量	451.161987
PSA	77.04000
LogP	4.53
蒸汽压	0.0±2.3 mmHg at 25°C
折射率	1.668

4-氯吡咯并嘧啶 3680-69-1 ~% 7-甲基-5-[1-[[3-(... 1337531-36-8
文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207
5-溴二氢吲哚 22190-33-6 ~%	文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207
1-BOC-吲哚啉-5-硼酸频那醇酯 837392-67-3 ~%	文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207
N-BOC-5-溴吲哚啉 261732-38-1 ~%	文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207
4-氯-7-甲基吡咯并[2,3-D]嘧啶 7781-10-4 ~% 7-甲基-5-[1-[[3-(... 1337531-36-8
文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207
5-溴-4-氯-7-甲基-7H… 1266343-30-9 ~% 7-甲基-5-[1-[[3-(... 1337531-36-8
文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207
5-溴-7-甲基-7h-吡咯并… 1337532-51-0 ~% 7-甲基-5-[1-[[3-(... 1337531-36-8
文献：Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207

上游产品? 7
CAS号1337532-51-0 5-溴-7-甲基-7h-吡咯并… CAS号3680-69-1 4-氯吡咯并嘧啶 CAS号22190-33-6 5-溴二氢吲哚 CAS号837392-67-3 1-BOC-吲哚啉-5-硼酸频那醇酯
CAS号261732-38-1 N-BOC-5-溴吲哚啉 CAS号7781-10-4 4-氯-7-甲基吡咯并[2,3-D]嘧啶 CAS号1266343-30-9 5-溴-4-氯-7-甲基-7H…
下游产品? 0

上游产品? 7