中文名称 | 1-(5-(4-氨基-7-甲基-7H-吡咯并[2,3-d]嘧啶-5-基)二氢吲哚-1-基)-2-(3-(三氟甲基)苯基)乙酮 |
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英文名称 | 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone;GSK2606414 (Synonyms: GSK 2606414) |
CAS号 | 1337531-36-8 |
分子式 | C24H20F3N5O |
分子量 | 451.44 |
外观 | White powder |
储存条件 | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM. It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Because PERK mediates the unfolded protein response pathway, which has roles in neurotoxicity and cancer, inhibition of PERK signaling has potential applications for the treatment of cancer and also cognitive degeneration.
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