CC-223 is an orally available inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR, a serine/threonine kinase that is upregulated in a variety of tumors, plays an important role downstream in the PI3K/AKT/mTOR signaling pathway, which is frequently dysregulated in human cancers.
1: Bendell JC, Kelley RK, Shih KC, Grabowsky JA, Bergsland E, Jones S, Martin T, Infante JR, Mischel PS, Matsutani T, Xu S, Wong L, Liu Y, Wu X, Mortensen DS, Chopra R, Hege K, Munster PN. 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. doi: 10.1002/cncr.29422. Epub 2015 Jul 15. PubMed PMID: 26177599.
2: Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. J Med Chem. 2015 Jul 9;58(13):5323-33. doi: 10.1021/acs.jmedchem.5b00626. Epub 2015 Jun 26. PubMed PMID: 26083478.
3: Mortensen DS, Fultz KE, Xu S, Xu W, Packard G, Khambatta G, Gamez JC, Leisten J, Zhao J, Apuy J, Ghoreishi K, Hickman M, Narla RK, Bissonette R, Richardson S, Peng SX, Perrin-Ninkovic S, Tran T, Shi T, Yang WQ, Tong Z, Cathers BE, Moghaddam MF, Canan SS, Worland P, Sankar S, Raymon HK. CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization. Mol Cancer Ther. 2015 Jun;14(6):1295-305. doi: 10.1158/1535-7163.MCT-14-1052. Epub 2015 Apr 8. PubMed PMID: 25855786.
4: Ashworth RE, Wu J. Mammalian target of rapamycin inhibition in hepatocellular carcinoma. World J Hepatol. 2014 Nov 27;6(11):776-82. doi: 10.4254/wjh.v6.i11.776. Review. PubMed PMID: 25429315; PubMed Central PMCID: PMC4243151.
(last updated: 4/19/2016)
Chemical |
CAS Num |
1228013-30-6 |
Chemical Formula |
C21H27N5O3 |
Molecular Weight |
397.48 |
IUPAC Chemical Name |
7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((1r,4r)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one |
Exact Mass |
397.21139 |
Elemental Analysis |
C, 63.46; H, 6.85; N, 17.62; O, 12.08 |
Synonym |
CC-223; CC 223; CC223. |
Solubility |
Soluble in DMSO, not in water |
SMILES Code |
OC(C)(C)C(N=C1)=CC=C1C(N=C2N3[C@@H]4CC[C@H](CC4)OC)=CN=C2NCC3=O |
Biological |
Targets and Effects |
mTOR inhibitor |
Pathways |
Apoptosis |
Physical |
Appearance |
Solid powder |
Purity |
>98% (or refer to the Certificate of Analysis) |
Shipping Condition |
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition |
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life |
>2 years if stored properly |