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- 文献和实验
- 技术资料
- CAS号：
1228013-30-6
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥286.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥554.0 |
| 规格： | 5mg | 产品价格： | ￥634.0 |
| 规格： | 10mg | 产品价格： | ￥1056.0 |
| 规格： | 25mg | 产品价格： | ￥1888.0 |
| 规格： | 50mg | 产品价格： | ￥2920.0 |
| 规格： | 100mg | 产品价格： | ￥4104.0 |
| 规格： | 200mg | 产品价格： | ￥5704.0 |
Product Introduction
Bioactivity
| 名称 | Onatasertib |
| 描述 | Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM). |
| 细胞实验 | Compound is spotted via an acoustic dispenser (EDC ATS-100) into an empty 384-well plate. Cells are diluted to desired densities and added directly to the compound-spotted plates. Cells are allowed to grow for 72 hours. Viability is assessed via Cell Titer-Glo. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as GI50 and/or IC50 values.(Only for Reference) |
| 激酶实验 | Kinase assays mTOR.: Reagents are prepared as follows:"Simple Tor buffer": 10 mM Tris pH 7.4, 100 mM NaCl, 0.1% Tween-20, 1 mM DTT. Recombinant mTOR is diluted in this buffer to an assay concentration of 0.200ug/mL. ATP/Substrate solution: 0.075 mM ATP, 12.5 mM MnCl2, 50 mM Hepes, pH 7.4, 50 mM β-GOP, 250 nM Microcystin LR, 0.25 mM EDTA, 5 mM DTT, and 3.5 μg/mL GST-p70S6. Dilution Curve: A 10-point, 1:3 dilution of compounds are prepared in neat DMSO at 50 times the final assay concentration. Detection reagent mix: 50 mM HEPES, pH 7.4 0.01% Triton X-100, 0.01% BSA, 0.1 mM EDTA, 12.7 ug/mL Cy5-anti-GST antibody, 9 ng/ml anti-phospho p70S6 antibody (Thr389), 627ng/mL anti-mouse IgG labeled with Lance Eu. To 20 uL of the Simple Tor buffer is added 0.5 uL of the compound Dilution Curve in DMSO. The final concentration range for compound is 30 to 0.0015 μM. To initiate the reaction, 5 μL of the ATP/substrate solution is added to the above. The reaction is allowed to run for 60 minutes. The assay is stopped by adding 5 μL of 60 mM EDTA. Ten (10) μL of detection reagent mix is then added, and the mixture is allowed to sit at least 2 hours before reading on a Perkin Elmer Envision microplate reader set to detect Europium-based TR-FRET. |
| 体外活性 | 在PC-3肿瘤移植的小鼠中,CC-223 (25 mg/kg,p.o.)抑制了mTORC1和mTORC2的活性.CC-223 (25 mg/kg, p.o.)还抑制了许多肿瘤模型的肿瘤生长,包括前列腺癌,神经胶质瘤,乳腺癌,肺癌以及结肠癌模型（47%-95%）. |
| 体内活性 | 在许多的细胞系中,CC-223对mTORC1 (S6RP and 4EBP1)和mTORC2 [AKT(S473)]标记物均有抑制作用,其IC50为pAKT（S473,11-150 nM）,pS6RP（27-184 nM）,p4EBP1（120-1050 nM）。CC-223还对许多癌细胞系的生长有抑制作用并诱导它们凋亡。 |
| 存储条件 | Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 125 mg/mL (314.49 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.03 mM), Sonication is recommended. Ethanol : 73 mg/mL (183.66 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | PI3K-α | Onatasertib | mTOR | Mammalian target of Rapamycin | Inhibitor | inhibit | FLT4 | DNA-PK | DNAPK | c-Fms | cFms | ATG-008 | ATG008 | ATG 008 | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 CC223【1228013-30-6】
￥286 - 5704
