中文名 | PF-4708671 |
英文名 | PF-4708671 |
别名 | P70核糖体S6激酶1抑制剂(S6K1抑制剂)(PF-4708671) 2-[[4-(5-乙基-4-嘧啶基)-1-哌嗪基]甲基]-6-(三氟甲基)-1H-苯并咪唑 2-((4-(5-乙基嘧啶-4-基)哌嗪-1-基)甲基)-6-(三氟甲基)-1H-苯并[D]咪唑 |
英文别名 | PF 4708671 PF-4708671 PF-04708671 2-[[4-(5-ethyl-4-pyriMidinyl)-1-piperazinyl]Methyl]-6-(trifluoroMethyl)-1H-benziMidazole 2-[[4-(5-ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-6-(trifluoromethyl)-1H-benzimidazole 1H-Benzimidazole, 2-[[4-(5-ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)- 2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole 2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671 |
CAS | 1255517-76-0 |
化学式 | C19H21F3N6 |
分子量 | 390.41 |
溶解度 | DMSO: ≥ 20 mg/mL |
存储条件 | room temp |
外观 | 粉末 |
颜色 | off-white |
MDL号 | MFCD18086922 |
体外研究 | PF-4708671是一种哌嗪基嘧啶类似物,是第一个S6K1特异性抑制剂。PF-4708671不显著抑制紧密相关的S6K2亚型或一组其他AGC激酶 (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 或SGK1)的活性。PF-4708671抑制S6K1介导的响应IGF-1(胰岛素样生长因子1)的S6蛋白的磷酸化,对PMA-诱导的底物磷酸化没有作用效果,底物与RSK (p90核糖体S6激酶)和MSK(丝分裂原和应激活化蛋白激酶)激酶高度相关。PF-4708671诱导S6K1的T型环和疏水性基序磷酸化,这种作用依赖于mTORC1 (mTOR复合体1)。PF-4708671不影响mTORC1的活性。 |
体内研究 | The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment. |
危险品标志 | T - 有毒物品 |
风险术语 | 25 - 吞食有毒。 |
安全术语 | 45 - 若发生事故或感不适,立即就医(可能的话,出示其标签)。 |
危险品运输编号 | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
参考资料 展开查看 | 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 配置溶液浓度参考:1mg5mg10mg1 mM2.561 ml12.807 ml25.614 ml5 mM0.512 ml2.561 ml5.123 ml10 mM0.256 ml1.281 ml2.561 ml50 mM0.051 ml0.256 ml0.512 ml 保存条件: -20℃ PF-4708671 is a novel cell-permeable inhibitor of S6K1 (p70 ribosomal S6 kinase 1), with a Ki of 20 nM and IC50 of 160 nM. IC50 Value: 160 nM [1] Target: S6K1 PF-4708671 is a novel cell-permeable inhibitor of S6K1, which specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM. PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 was also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 is the first S6K1-specific inhibitor to be reported and will be a useful tool for delineating S6K1-specific roles downstream of mTOR [1]. |
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