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PP121  ≥98%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（20 mg/mL 超声）
产品描述：基本信息 产品编号： P10814 产品名称： PP121 CAS: 1092788-83-4   储存条件 粉末 -20℃ 四年     分子式： C17H17N7 溶于液体 -80℃ 6个月 分子量： 319.36 -20℃ 1个月 化学名：  PP121;1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Solubility (25°C)：   体外:   DMSO 64mg/mL (200.4mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2mg/mL(6.26mM);Clear solution 此方案可获得 ≥ 2 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2.请依序添加每种溶剂：10% DMSO→90%(20% SBE-β-CD in saline) Solubility:≥2mg/mL(6.26mM);Clear solution 此方案可获得 ≥ 2 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2mg/mL(6.26mM);Clear solution 此方案可获得 ≥ 2 mg/mL (6.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 ＜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 3.1313mL 15.6563mL 31.3126mL 5mM 0.6263mL 3.1313mL 6.2625mL 10mM 0.3131mL 1.5656mL 3.1313mL   生物活性 产品描述 是多靶点激酶抑制剂，抑制mTOR，DNK-PK，VEGFR2，Src，PDGFR的IC50值分别为10，60，12，14，2nM。 靶点 mTOR;PDGFR;VEGFR;Src;Apoptosis 体外研究 PP121 blocks the PI3K pathway by direct inhibition of PI3K/mTOR in two glioblastoma cell lines,U87 and LN229.PP121 potently inhibits the proliferation of a diverse panel of tumor cell lines containing mutations in the PI3-K pathway components PIK3CA,PTEN,or RAS.PP121 induces a G0G1 arrest in most tumor cells.PP121 directly inhibits Src in cells and reverses its biochemical and morphological effects.PP121 potently inhibits the Ret kinase domain in vitro (IC50<1nM).PP121 potently blocks VEGF stimulated activation of the PI3-K and MAPK pathways.PP121 inhibits VEGFR2 autophosphorylation at low nanomolar concentrations,confirming that this molecule directly targets VEGFR2 in cells.PP121 inhibits Bcr-Abl induced tyrosine phosphorylation in K562 cells as well as BaF3 cells that express Bcr-Abl. 体内研究 Oral administration of PP121 remarkably inhibits Eca-109 xenograft growth.Mice body weights are not significantly affected by PP121 or the vehicle treatment.PP121 oral administration dramatically inhibits activations of Akt-mTOR and NFkB in xenograft tumors.p-Akt Ser 473 and p-IKKa/b are both inhibited by PP121 administration.   推荐实验方法(仅供参考) 激酶实验： Purified kinase domains are incubated with inhibitors (PP121) at 2-or 4-fold dilutions over a concentration range of 50-0.001µM or with vehicle (0.1% DMSO) in the presence of 10µM ATP,2.5µCi of γ- 32P-ATP and substrate.Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes,depending on the substrate;this membrane is then washed 5-6 times to remove unbound radioactivity and dried.Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software.   细胞实验:   Cells grown in 96-well plates are treated with PP121 at 4-fold dilutions (10µM-0.040μM) or vehicle (0.1% DMSO).After 72h cells are exposed to Resazurin sodium salt (22µM) and fluorescence is quantified.IC50 values are calculated.For proliferation assays involving single cell counting,non-adherent cells are plated at low density (3–5% confluence) and treated with drug (2.5µM) or vehicle (0.1% DMSO).Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer.   动物实验:   Mice:Eca-109 cells are injected into the axillary regions of nude mice (5×106 cells/mouse).When the tumor volumes reach around 200 mm3,the mice are randomly separated to three groups:Untreated control,PP121 (30mg/kg) and vehicle (10% 1-methyl-2-pyrrolidinone and 90% PEG 300) group.Tumor volumes and the mice body weights are measured every 10 d.
保存条件：-20℃

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