Onatasertib (CC 223)

製品コードS7886 バッチS788601

印刷

化学情報

Chemical Structure Synonyms ATG-008 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H27N5O3
分子量 397.47 CAS No. 1228013-30-6
Solubility (25°C)* 体外 DMSO 79 mg/mL (198.75 mM)
Ethanol 79 mg/mL (198.75 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Onatasertib (CC 223) is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2.
in vitro In a panel of cell lines, CC-223 inhibits both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers with IC50 ranges of 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1 and 11 to 150 nM for pAKT(S473), respectively. CC-223 also inhibits cell growth and induces apoptosis across a number of cancer cell lines. [1]
in vivo In PC-3 tumor-bearing mice, CC-223 (25 mg/kg, p.o.) inhibits both mTORC1 and mTORC2. CC-223 (25 mg/kg, p.o.) also results in tumor growth inhibition by 47% to 95% in xenograft models of prostate, glioma, breast, lung, and colon. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assays mTOR.
Reagents are prepared as follows:”Simple Tor buffer”: 10mM Tris pH 7.4, 100mM NaCl, 0.1% Tween-20, 1mM 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, 50mM 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.
細胞アッセイ 細胞株 PC-3, CAL-51, A549,T47D,NCI-H460, HepG2, AU565, Hep3B, HCC, U87MG, HCT116, MDA-MB-231, and NCI-H23 cells
濃度 ~ 10 μM
反応時間 72 h
実験の流れ 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.
動物実験 動物モデル Mice bearing PC-3, U-87 MG, HCT 116, MDA-MB-231, or A549 tumors
投薬量 25 mg/kg
投与方法 p.o.

カスタマーフィードバック

Data from [Data independently produced by , , PLoS One, 2017, 12(3):e0173252. ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CC-223 inhibits human head and neck squamous cell carcinoma cell growth [Wang JY Biochem Biophys Res Commun, 2018, 496(4):1191-1196] PubMed: 29402408
CC-223 blocks mTORC1/C2 activation and inhibits human hepatocellular carcinoma cells in vitro and in vivo [Xie Z PLoS One, 2017, 12(3):e0173252] PubMed: 28334043

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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