GSK 2606414

Cat. No. 5107 16 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective PERK inhibitor; orally bioavailable

化学名： 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone

纯度： ≥99% (HPLC)

引用文献 (16)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GSK 2606414

GSK 2606414 is a potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC₅₀ = 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Orally bioavailable.

许可信息

Sold for research purposes only under agreement from GlaxoSmithKline

化合物库 for GSK 2606414

GSK 2606414 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for GSK 2606414

分子量	451.44
公式	C₂₄H₂₀F₃N₅O
储存	Store at -20°C
纯度	≥99% (HPLC)
CAS Number	1337531-36-8
PubChem ID	53469448
InChI Key	SIXVRXARNAVBTC-UHFFFAOYSA-N
Smiles	NC1=NC=NC2=C1C(C3=CC(CCN4C(CC5=CC=CC(C(F)(F)F)=C5)=O)=C4C=C3)=CN2C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for GSK 2606414

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	45.14	100

制备储备液 for GSK 2606414

以下数据基于产品分子量 451.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.22 mL	11.08 mL	22.15 mL
5 mM	0.44 mL	2.22 mL	4.43 mL
10 mM	0.22 mL	1.11 mL	2.22 mL
50 mM	0.04 mL	0.22 mL	0.44 mL

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产品说明书 for GSK 2606414

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GSK 2606414

参考文献是支持产品生物活性的出版物。

Axten et al (2012) 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 reticulum kinase (PERK). J.Med.Chem. 55 7193 PMID: 22827572

Harding et al (2012) Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK. J.Biol.Chem. 287 44338 PMID: 23148209

If you know of a relevant reference for GSK 2606414, please let us know.

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关键词: GSK 2606414, GSK 2606414 supplier, GSK2606414, potent, selective, protein, kinase, R-like, ER, PERK, orally, bioavailable, antitumor, ER-stress, 5107, Tocris Bioscience