Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Onatasertib (CC223) 是一种口服有效的mTOR 激酶抑制剂,抑制mTOR 激酶,IC50为 16 nM。它抑制mTORC1和mTORC2。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 378 | 现货 | ||
2 mg | ¥ 588 | 现货 | ||
5 mg | ¥ 980 | 现货 | ||
10 mg | ¥ 1,560 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,390 | 现货 | ||
100 mg | ¥ 6,180 | 现货 | ||
500 mg | ¥ 12,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 869 | 现货 |
产品描述 | 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). |
靶点活性 | mTOR:16 nM |
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。 |
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 | CC223, CC 223, CC-223 |
分子量 | 397.47 |
分子式 | C21H27N5O3 |
CAS No. | 1228013-30-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 73 mg/mL (183.7 mM)
Ethanol: 73 mg/mL (183.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.5159 mL | 12.5796 mL | 25.1591 mL | 62.8978 mL |
5 mM | 0.5032 mL | 2.5159 mL | 5.0318 mL | 12.5796 mL | |
10 mM | 0.2516 mL | 1.258 mL | 2.5159 mL | 6.2898 mL | |
20 mM | 0.1258 mL | 0.629 mL | 1.258 mL | 3.1449 mL | |
50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.258 mL | |
100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.629 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Onatasertib 1228013-30-6 Angiogenesis Apoptosis DNA Damage/DNA Repair PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors c-Fms DNA-PK FLT PI3K mTOR ATG008 Mammalian target of Rapamycin inhibit ATG-008 Inhibitor CC223 CC 223 ATG 008 CC-223 inhibitor