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Acalisib  ≥98%（HPLC）

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(≥29mg/mL)
产品描述：基本信息 产品编号： A10103  产品名称： Acalisib CAS: 870281-34-8   储存条件 粉末 -20℃ 四年 分子式： C21H16FN7O 溶于液体 -80℃ 6个月 分子量： 401.40 -20℃ 1个月 化学名：  (S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one Solubility (25°C)：   体外:   DMSO 80mg/mL (199.3mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照In Vitro⽅式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐是指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(6.23mM);Clear solution 2.请依序添加每种溶剂：10% DMSO→90%(20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(6.23mM);Clear solution 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(6.23mM);Clear solution ＜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 2.4913mL 12.4564mL 24.9128mL 5mM 0.4983mL 2.4913mL 4.9826mL 10mM 0.2491mL 1.2456mL 2.4913mL   生物活性 产品描述 一种PI3K的β和δ异构体抑制剂，IC5:12.7nM,具有潜在的免疫调节和抗肿瘤活性。 靶点 PI3K 体外研究 Acalisib (GS-9820) is more selective for PI3Kδ(IC50=12.7nM) relative to other PI3K class I enzymes (IC50:PI3Kα,5,441nM;PI3Kβ,3,377nM;PI3Kγ,1,389nM).Acalisib is also 103-fold more selective against PI3Kδthan against related kinases,such as PI3KCIIβ(IC50>10nM),hVPS34 (IC50=12.7μM),DNA-PK (IC50=18.7μM),and mTOR (IC50>10nM).In fibroblasts,the PDGF receptor signals through PI3Kαand the GPCR for lysophosphatidic acid (LPA) signals through PI3Kβ.Acalisib reduces PDGFinduced pAkt by only 50% at 11,585nM,and LPA-induced pAkt by 50% at 2,069nM. 体内研究 To dissect the relative contribution of PI3Kαand PI3Kδinhibition in the reduction of obesity,obese hyperphagic ob/ob mice are treated with a selective PI3Kαinhibitor,BYL-719,or with a selective PI3Kδinhibitor,Acalisib (GS-9820).Remarkably,BYL719 reduces body weight after 15 days of treatment to a similar extent as CNIO-PI3Ki,whereas Acalisib has no significant effect at the same doses as BYL-719.It should be noted that 10mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice.   推荐实验方法(仅供参考) 激酶实验： Biochemical in vitro lipid kinase assays are performed.A stock solution of Acalisib (GS-9820) is prepared in DMSO at a concentration of 10mM.Ten-point kinase inhibitory activities are measured over a concentration range (5 to 104nM) with ATP at a concentration consistent with the Km of each of the enzymes.   细胞实验:   The effect of inhibitors on RAW264.7 cell survival is evaluated using the MTT assay.RAW264.7 cells are seeded in Falcon flat bottom 96-well plates at a density of 2.5-3×104 cells/cm2 in 100μL of DMEM with 10% FBS and 1% antibiotic solution.After seeding,the cells are allowed to attach for 24h then exposed to control or Acalisib (GS-9820) (100 pM to 10μM) for 24h.After incubation at 37℃ in 5% CO2,MTT substrate is added at a final concentration of 0.5mg/mL for 4h.Following a 4-h incubation,100μL of solubilization solution is added to each well to dissolve the formazan crystals and samples are analyzed after 24h. Absorbance of the samples is assessed using a plate reader using a wavelength of 550nm and a reference wavelength of 700nm.   动物实验:   Mice Ob/ob C57BL6J mice and Wild-type C57BL6J/Ola.Hsd mice are housed under specific pathogen free (SPF) conditions,at 22℃,and with 12 hours dark/light cycles (light cycle from 8 am to 8 pm).All mice used are males of 20 weeks of age.Mice are fed with standard chow diet (18% of fat-based caloric content).PI3K inhibitors are administered daily by oral gavage during 15 or 16 days as follows,BYL-719 (5 and 10mg/kg) and Acalisib (5 and 10mg/kg),CNIO-PI3Ki (1 and 5mg/kg),dissolved in PEG-300 and 10% N-methyl-2-pyrrolidone.
保存条件：-20℃

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