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PF-4708671  ≥98%

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包装规格：10mg 50mg in glass bottle
溶解性：溶于DMSO（33.33 mg/mL 超声）
产品描述：基本信息 产品编号：P10866 产品名称：PF-4708671 CAS: 1255517-76-0   储存条件 粉末 -20℃ 四年     分子式： C19H21F3N6 溶于液体 -80℃ 两年 分子量 390.41 -20℃ 一个月 化学名：  2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole   Solubility (25°C)   体外 DMSO 30mg/mL (76.84mM) Ethanol 40mg/mL (102.45mM) Water Insoluble 体内（现配现用） 30% PEG400+0.5% Tween80+5% propylene glycol 30mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5614mL 12.8070mL 25.6141mL 5mM 0.5123mL 2.5614mL 5.1228mL 10mM 0.2561mL 1.2807mL 2.5614mL 50mM 0.0512mL 0.2561mL 0.5123mL   生物活性 产品描述 一种有效的细胞渗透性 S6K1 抑制剂，Ki为 20nM，IC50 为 160nM。 靶点/IC50 p70 S6K1 (Cell-free assay) 160nM   体外研究 PF-4708671 inhibits the activity of full-length S6K1 in vitro with a Ki of 20nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with an IC50 of 0.16μM, and only inhibits very weakly the closely related S6K2 isoform (IC50 of 65μM). PF4708671 inhibits RSK1 (IC50 of 4.7μM) and RSK2 (IC50 of 9.2μM) over 20-fold less potently than S6K1. PF4708671 inhibits MSK1 (IC50 of 0.95μM) 4-fold more weakly than S6K1[1]. HCT116 cells are treated with (i) vehicle (DMSO), (ii) OSI-906 (5μM), (iii) PF-4708671 (10μM), and (iv) OSI-906 (5μM)+PF-4708671 (10μM) for various amounts of time. HCT116 cells treated with OSI-906 alone (closed square) or PF4708671 alone (open circle) slightly inhibit cell growth. In contrast, proliferation in HCT116 cells is significantly inhibited after a 2-day treatment with the combination of OSI-906 and PF-4708671 (closed circle). A similar result is also observed when SW480 cells are treated with the combination of OSI-906 and PF-4708671.Colony formation also significantly reduces in OSI-906+PF-4708671-treated cells comparing with vehicle, OSI-906 alone, or PF-4708671 alone treated HCT116 or SW480 cells.   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 OSI906 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.   推荐实验方法(仅供参考) 细胞实验： Cell Assay GEO, HT29, SW480, and HCT116 cells are used. The effects of OSI-906 or the combination of OSI-906 and PF-4708671 on cell proliferation is determined with XTT and clonogenic assays. XTT assays are performed using the Cell Proliferation Kit II (XTT). For clonogenic assays, cells (1×103 cells/well) are seeded on a 6-well plate and subsequently treated with drugs (OSI906 5μM, PF-4708671 10μM). After 1 week of incubation, cells are stained with 1% crystal violet, and the number of colonies is counted and recorded.   动物实验:   Animal Administration Mice Five- to 6-week-old female athymic nude mice (Hsd:Athymic Nude-Foxn1nu) are randomly assigned to the following groups(5 mice/group). For injection of HT29-L and HT29-P cells, mice are treated with vehicle (25mM tartaric acid) or OSI-906 (30mg/kg) for 12 days. For injection of HCT116 cells, mice are treated with (i) vehicle (25mM tartaric acid); (ii) OSI-906 alone (30mg/kg); (iii) PF-4708671 alone (60mg/kg); and (iv) OSI-906 (30mg/kg)+PF-4708671 (60mg/kg) and treated with drugs orally for 14 days. Vehicle and OSI-906 are given once per day and PF-4708671 is given once every other day. Twenty-four hours after the last treatment, the mice are sacrificed and the tumor weights were measured.
保存条件：-20℃

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