Sapanisertib (INK 128, MLN0128,TAK-228)
目录号：S2811
Molecular Weight(MW): 309.33
Sapanisertib (INK 128, MLN0128) 是一种有效的，选择性mTOR抑制剂，在无细胞试验中IC50为1 nM；对I型PI3K亚型的作用效果低200倍以上，与Rapamycin相比，优先抑制mTORC1/2，且对促侵袭基因敏感。Phase 1。
客户使用该产品的5个实验数据：
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Blockade of PD-1 in combination with INK128 inhibits liver cancer cell proliferation and clone formation in vitro in immunocompetent mice. (A) Representative pictures show the clone formation of different administered groups in SMMC7721 PD-1 OE cells. (B) Histogram showing mean number of cloned formed 6 SD in each group. P < 0.05. (C) Optical density values 6 SD of Cell Counting Kit 8 assay in different administered groups in SMMC7721 PD-1 OE cells. (D,E) Flow-cytometric assessment of cell death with percent of annexin V1/7-aminoactinomycin D1 cells, mean 6 SEM. (F,G) Tumor growth kinetics (mean±SD) of different administered groups versus corresponding control in C57BL/6 mice subcutaneously implanted with PD-1 OE or vector-control Hepa1-6 cells. *P < 0.5; **P < 0.01; ***P < 0.001; #, not significant. Abbreviations: 7-AAD, 7-aminoactinomycin D; CCK8, Cell Counting Kit 8; NS, not significant; OD, optical density.
Hepatology, 2017, 66(6):1920-1933. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
Hep-2 (D) or SCC-9 (E) cells were treated with PI3K/Akt and mTOR dual inhibitor LY 294002 (LY, 1 umol/L), mTORC1 inhibitor rapamycin (0.5 umol/L), mTORC1/2 dual inhibitor AZD2014 (0.1 uM), INK-128 (0.1 uM) or AZD8055 (0.1 uM) for 72 h, cell viability was analyzed. The mean of three independent experiments performed in triplicate was shown. Statistical significance was analyzed by ANOVA. *p < 0.01 vs Control. **p < 0.01 vs. AZD8055 group.
Biochem Biophys Res Commun 2013 440(4), 701-6. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
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(A–C), BMDMs were pretreated with or without INK128 (10, 20, or 30 nM) for 1 h and primed with LPS for 3 h. The cells were then stimulated with or without ATP. (A) Western blot analysis of IL-1β and cleaved caspase-1 in the supernatants and western blot analysis of NLRP3, pro-caspase-1 and pro-IL-1β in the lysates.
Acta Biochim Biophys Sin (Shanghai), 2018, doi: 10.1093/abbs/gmy088. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
Antonino Maria Spart from University of Bologn. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
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Bone marrow derived macrophages were pre-treated with 1nM INK128 for 1h prior to LPS treatment (100 ng/ml). TNF-a production was analyzed 24h later.
Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
产品安全说明书
mTOR抑制剂选择性比较
生物活性
| 产品描述 | Sapanisertib (INK 128, MLN0128) 是一种有效的，选择性mTOR抑制剂，在无细胞试验中IC50为1 nM；对I型PI3K亚型的作用效果低200倍以上，与Rapamycin相比，优先抑制mTORC1/2，且对促侵袭基因敏感。Phase 1。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 靶点 |
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| 体外研究 |
INK 128 表现对mTOR酶的抑制活性并对PI3K激酶的选择性超过100倍。[1] 作为TORC1/2抑制剂，INK 128抑制TORC1的下游底物S6和4EBP1的磷酸化。此外，INK 128也显示了对雷帕霉素和泛PI3K抑制剂耐受的细胞株的有效抑制效应。[2] |
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| Cell Data |
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| 体内研究 | 在ZR-75-1乳腺癌异种移植模型中，INK 128（0.3 mg/kg/day）的处理表现了肿瘤生长抑制效果。[1] 在多种移植体模型中，每日口服给药INK 128抑制血管生成和肿瘤生长。[2] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
溶解度 (25°C)
| 体外 | DMSO | 62 mg/mL (200.43 mM) |
|---|---|---|
| Ethanol | 2 mg/mL (6.46 mM) | |
| Water | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 30% PEG400+0.5% Tween80+5% propylene glycol |
30 mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 309.33 |
|---|---|
| 化学式 | C15H15N7O |
| CAS号 | 1224844-38-5 |
| 稳定性 | powder |
| in solvent | |
| 别名 | N/A |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02575339 | Active not recruiting | Hepatocellular Carcinoma|Liver Cancer|HCC | Bert O''Neil MD|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium | July 2016 | Phase 1|Phase 2 |
| NCT02756364 | Active not recruiting | Breast Neoplasms | Millennium Pharmaceuticals Inc.|Takeda | June 1 2016 | Phase 2 |
| NCT02724020 | Active not recruiting | Clear-cell Metastatic Renal Cell Carcinoma | Millennium Pharmaceuticals Inc.|Takeda | June 30 2016 | Phase 2 |
| NCT02719691 | Recruiting | Metastatic Breast Cancer|Solid Tumors | University of Colorado Denver | May 13 2016 | Phase 1 |
| NCT02725268 | Recruiting | Endometrial Neoplasms | Millennium Pharmaceuticals Inc.|European Network of Translational Research in Ovarian Cancer - EUTROC|European Network of Individualized Treatment in Endometrial Cancer - ENITEC|Takeda | April 1 2016 | Phase 2 |
| NCT02514824 | Active not recruiting | Merkel Cell Carcinoma | Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. | October 2015 | Phase 1|Phase 2 |
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
常见问题及建议解决方法
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问题 1：
What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?
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回答：
You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.
