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- 2025年07月23日
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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Acalisib
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
870281-34-8
- 规格：
100mg/50mg/25mg/10mg/1mg/5mg
| 规格： | 100mg | 产品价格： | ￥2428.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥1728.0 |
| 规格： | 25mg | 产品价格： | ￥1078.0 |
| 规格： | 10mg | 产品价格： | ￥586.0 |
| 规格： | 1mg | 产品价格： | ￥206.0 |
| 规格： | 5mg | 产品价格： | ￥386.0 |
是一种具有高度选择性的、有效的p110δ抑制剂。
| 基本信息 | |
| CAS | No.870281-34-8 |
| 英文名称 | Acalisib |
| 别名 | GS-9820;CAL-120 |
| 分子式 | C21H16FN7O |
| 分子量 | 401.4 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 604-604-1 |
| SMILES | O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)C)=NC5=C1C=C(F)C=C5 |
| 靶点 | PI3K |
| 通路 | PI3K/Akt/mTOR |
| 背景说明 | 是一种具有高度选择性的、有效的p110δ抑制剂。 |
| 生物活性 | Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.[1-2] |
| In Vitro | Acalisib(GS-9820)is more selective for PI3Kδ(IC50=12.7 nM)relative to other PI3K class I enzymes(IC50: PI3Kα，5，441 nM; PI3Kβ，3，377 nM; PI3Kγ，1，389 nM). Acalisib is also 103-fold more selective against PI3Kδ than against related kinases，such as PI3KCIIβ(IC50>10 nM)，hVPS34(IC50=12.7 μM)，DNA-PK(IC50=18.7 μM)，and mTOR(IC50>10 nM). In fibroblasts，the PDGF receptor signals through PI3Kα and the GPCR for lysophosphatidic acid(LPA)signals through PI3Kβ. Acalisib reduces PDGF-induced pAkt by only 50% at 11，585 nM，and LPA-induced pAkt by 50% at 2，069 nM.[1] |
| 细胞实验 | To dissect the relative contribution of PI3Kα and PI3Kδ inhibition in the reduction of obesity，obese hyperphagic ob/ob mice are treated with a selective PI3Kα inhibitor，BYL-719，or with a selective PI3Kδ inhibitor，Acalisib(GS-9820). Remarkably，BYL-719 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 10 mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice[2]. |
| 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 100 μL of DMEM with 10% FBS and 1% antibiotic solution. After seeding，the cells are allowed to attach for 24 h then exposed to control or Acalisib(GS-9820)(100 pM to 10 μM)for 24 h. After incubation at 37°C in 5% CO2，MTT substrate is added at a final concentration of 0.5 mg/mL for 4 h. Following a 4-h incubation，100 μL of solubilization solution is added to each well to dissolve the formazan crystals and samples are analyzed after 24 h. Absorbance of the samples is assessed using a plate reader using a wavelength of 550 nm and a reference wavelength of 700 nm[1]. |
| 动物实验 | Ob/ob C57BL6J mice and Wild-type C57BL6J/Ola.Hsd mice are housed under specific pathogen free(SPF)conditions，at 22°C，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 10 mg/kg)and Acalisib(5 and 10 mg/kg)，CNIO-PI3Ki(1 and 5 mg/kg)，dissolved in PEG-300 and 10% N-methyl-2-pyrrolidone.[2] |
| 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 10 mM. Ten-point kinase inhibitory activities are measured over a concentration range(5 to 104 nM)with ATP at a concentration consistent with the Km of each of the enzymes[1]. |
| 数据来源文献 | [1]. Shugg RP， et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization， survival， and resorption. J Biol Chem. 2013 Dec 6;288(49):35346-57. [2]. Lopez-Guadamillas E， et al. PI3Kα inhibition reduces obesity in mice. Aging (Albany NY). 2016 Nov 4;8(11):2747-2753 |
| 单位 | 瓶 |
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IA2860 Acalisib 抑制剂/拮抗剂/激动剂 索莱宝
￥206 - 2428
