產品目錄

規格	5mg 25mg
CAS	1228013-30-6
別名
化學名	7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((1r,4r)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one
分子式	C21H27N5O3
分子量	397.47
溶解度	DMF: 30 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 25 mg/mL,Ethanol: 20 mg/mL
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產品描述：

CC-223 is an orally bioavailable mTOR inhibitor.

The mammalian target of rapamycin (mTOR) pathway is critical for tumor development, and mTOR inhibitors have revealed modest results.

In vitro: CC-223 was identified as an ATP–competitive inhibitor of the mTOR kinase targeting mTORC1 of both 4EBP1 and p70 S6 kinase 1 and mTORC2, which prevented the upregulation of AKT phosphorylation. Moreover, CC-223 was selectively potent to mTOR kinase while showed more than 150-fold sensitivity against the related lipid kinase, PI3Ka. In addition, CC-223 was active over many non-Hodgkin lymphoma cell lines and solid tumor lines such as including glioma, breast, hepatocellular carcinoma, as well as non–small cell lung cancer [1].

In vivo: In animal study, CC-223 was selected for evaluation in PC-3 tumor bearing efficacy mouse models. Mice were orally treated with vehicle or various doses of CC-223 once daily or twice daily at a dose of 5 mL/kg for 21 days, and the final reductions of tumor volume were measured following the final day of dosing. Results showed that All CC-223 had dose- and schedule-dependent inhibition of tumor growth in the PC-3 model. Moreover, the maximum observed efficacy for CC-223 was determined to be 87%, at its tolerated dose of 25 mg/kg q.d. [1].

Clinical trial: In previous clinical study, CC-223 was found to be tolerable with manageable toxicities. In addition, the preliminary antitumor activity, such as tumor regression and evidence of mTORC1/mTORC2 pathway inhibition were also observed [2].

References:

[1] Mortensen DS, et al. Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223. J Med Chem. 2015 Jul 9;58(13):5323-5333.

[2] Bendell JC, et al. A phase I dose-escalation study to assess safety, tolerability, pharmacokinetics, and preliminary efficacy of the dual mTORC1/mTORC2 kinase inhibitor CC-223 in patients with advanced solid tumors or multiple myeloma. Cancer. 2015 Oct 1;121(19):3481-90.

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原創作者：上海莼試生物技術有限公司

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賬戶名：上海生物

開戶行：中國銀行山東省分行營業部

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CC-223

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