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PF-4989216  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 29 mg/mL 超声）
产品描述：基本信息 产品编号： P10826 产品名称： PF-4989216 CAS: 1276553-09-3   储存条件 粉末 -20℃ 四年     分子式： C18H13FN6Os 溶于液体 -80℃ 6个月 分子量： 380.40 -20℃ 1个月 化学名：  4-(4-cyano-2-fluorophenyl)-2-morpholin-4-yl-5-(1H-1,2,4-triazol-5-yl)thiophene-3-carbonitrile Solubility (25°C)：   体外:   DMSO 76mg/mL (199.78mM) Ethanol 7mg/mL warmed with 50ºC water bath (18.4mM) Water Insoluble 体内(现配现用): Suspended in 0.5% methylcellulose 1mg/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 2.6288mL 13.1441mL 26.2881mL 5mM 0.5258mL 2.6288mL 5.2576mL 10mM 0.2629mL 1.3144mL 2.6288mL   生物活性 产品描述 一种有效的选择性PI3Kα抑制剂，Ki为0.6nM。 靶点 PI3Kα 0.6nM (Ki) Mtor 1440 nM (Ki) 体外研究 PF-4989216 (Compound 10) has excellent PI3KαKi (0.6nM),good cellular potency (S473 IC50=79nM),and good selectivity against mTOR (mTOR Ki=1440nM).PF-4989216 has PI3KαKi less than 1nM and mTOR Ki more than 1μM.PF-4989216 also has excellent selectivity over 40 other kinases,and no major CYP inhibitions are observed.Less than 30% inhibition is observed in 1A2,2C9,2D6,and 3A4 CYP enzymes at 3μM.The toxicity of PF-4989216 in several drug-sensitive and MDR cancer cell lines,including cells overexpressing ABCB1 or ABCG2,and in HEK293 cells transfected with human ABCB1 or ABCG2 is determined.PF-4989216 inhibits human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 with IC50s of 1.11±0.09 and 6.79±1.00uM,respectively.PF-4989216 inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 IC50s of 2.30±0.68,23.26±2.94 and 62.57±5.46uM,respectively.PF-4989216 inhibits pcDNA-HEK293,ABCB1-transected MDR19-HEK293,ABCG2-tranfected R482-HEK293 cells with IC50s of 0.44±0.05,0.38±0.06 and 5.05±0.89uM,respectively. 体内研究 PF-4989216 (Compound 10) is dosed orally in our in vivo antitumor model,PI3K driven NCI-H1975 xenograft tumors.PF4989216 demonstrates dose responsive tumor growth inhibitory activity from 25 to 200mg/kg in QD oral dosing.   推荐实验方法(仅供参考) 细胞实验:   MTT and CCK-8 assays are performed to determine the general sensitivities of cells to the tested drugs.The human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 are treated with PF-4989216 (0.1,1 and 10μM).The human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 are treated with PF-4989216 (0.1,1,10 and 100μM).The parental HEK293 and ABCG2-tranfected R482-HEK293 cells are treated with PF4989216 (0.01,0.1,1 and 10μM).For the reversal of cytotoxicity assays,PF-4989216 or Ko143 or Lapatinib at a nontoxic concentration is added into the cytotoxicity assay,and the extent of reversal is then calculated.   动物实验:   Mice For animal studies,6-8 week old nu/nu athymic female mice are used.Tumors are established by injecting 2×106 cells suspended 1:1 (v/v) with reconstituted basement membrane.For tumor growth inhibition studies,mice with established tumors of ~150 mm3 are randomized.PF-4989216 (Compound 10) is dosed orally (25,50,100 and 200mg/kg) in a mouse PI3K driven NCI-H1975 xenograft tumor model.Tumor dimensions are measured with vernier calipers,and tumor volumes are calculated.Tumor growth inhibition percentage (TGI%) is calculated.
保存条件：-20℃

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