| Identification | Back Directory | [Name]
2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-1-[2-(tetrahydro-2H-pyran-4-yl)ethyl]-6-[4-(1H-1,2,4-triazol-5-yl)phenyl]- | [CAS]
1021920-32-0 | [Synonyms]
2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-1-[2-(tetrahydro-2H-pyran-4-yl)ethyl]-6-[4-(1H-1,2,4-triazol-5-yl)phenyl]- | [Molecular Formula]
C20H21N7O2 | [MOL File]
1021920-32-0.mol | [Molecular Weight]
391.43 |
| Hazard Information | Back Directory | [Description]
CC214-1 is a novel dual mTORC1/mTORC2 inhibitor, inhibiting na?ve T cell activation and the expression of T-cell activation markers, inducing specific tolerance against alloantigens, while preserving anti-cytomegalovirus response. | [Uses]
CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy [1],with an IC50 is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study[2]. | [IC 50]
mTOR: 0.002 μM (IC50) | [References]
[1] Gini B, et al. The mTOR kinase inhibitors, CC214-1 and CC214-2, preferentially block the growth of EGFRvIII-activated glioblastomas. Clin Cancer Res. 2013 Oct 15;19(20):5722-32. DOI:10.1158/1078-0432.CCR-13-0527
[2] Mortensen DS, et al. Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91. DOI:10.1016/j.bmcl.2013.01.110
[3] Herrero-Sánchez MC, et al. Effect of mTORC1/mTORC2 inhibition on T cell function: potential role in graft-versus-host disease control. Br J Haematol. 2016 Jun;173(5):754-68. DOI:10.1111/bjh.13984 |
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