Onatasertib
作者：齊岳
發布時間：2023-08-23
09:20:17
點擊數：
產品名稱：Onatasertib
產品描述：
| 產品描述 | 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). |
| 靶點活性 | mTOR:16 nM |
| 體外活性 | 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.)還抑制了許多模型的生長,包括前列腺*,神經膠質瘤,乳腺*,肺*以及結腸*模型（47%-95%）. |
| 體內活性 | 在許多的細胞系中,CC-223對mTORC1 (S6RP and 4EBP1)和mTORC2 [AKT(S473)]標記物均有抑制作用,其IC50為pAKT（S473,11-150 nM）,pS6RP（27-184 nM）,p4EBP1（120-1050 nM）。CC-223還對許多*細胞系的生長有抑制作用并誘導它們凋亡。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | CC-223, CC 223, CC223 |
| 分子量 | 397.479 |
| 分子式 | C21H27N5O3 |
| CAS No. | 1228013-30-6 |
存儲
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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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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