Onatasertib
作者：齐岳
发布时间：2023-08-23
09:20:17
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产品名称：Onatasertib
产品描述：
| 产品描述 | CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. CC-223 is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM). |
| 靶点活性 | mTOR:16 nM |
| 体外活性 | 在PC-3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.)还抑制了许多模型的生长,包括前列腺*,神经胶质瘤,乳腺*,肺*以及结肠*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*细胞系的生长有抑制作用并诱导它们凋亡。 |
| 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. |
| 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) |
| 别名 | CC-223, CC 223, CC223 |
| 分子量 | 397.479 |
| 分子式 | C21H27N5O3 |
| CAS No. | 1228013-30-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 73 mg/mL (183.7 mM)
Ethanol: 73 mg/mL (183.7 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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