| Identification | Back Directory | [Name]
CC-115 | [CAS]
1228013-15-7 | [Synonyms]
CC-115
CS-2038
CC115;CC 115
CC-115, >95%
CC-115(free base)
1-Ethyl-7-(2-methyl-6-(4h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-5-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one
Pyrazino[2,3-b]pyrazin-2(1H)-one, 1-ethyl-3,4-dihydro-7-[2-methyl-6-(1H-1,2,4-triazol-5-yl)-3-pyridinyl]- | [Molecular Formula]
C16H16N8O | [MDL Number]
MFCD29036965 | [MOL File]
1228013-15-7.mol | [Molecular Weight]
336.35 |
| Chemical Properties | Back Directory | [Boiling point ]
587.3±60.0 °C(Predicted) | [density ]
1.56±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥50 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O | [form ]
solid | [pka]
5.94±0.20(Predicted) | [color ]
Pink to red |
| Hazard Information | Back Directory | [Biological Activity]
cc-115 is a inhibitor of mtor/dna-pk.the mammalian target of rapamycin (mtor) kinase is a key mediator of the phosphoinositide 3-kinase /protein kinase b (akt pathway). the dna-dependent protein kinase (dna-pk) is a critical component of the dna repair machinery governings the response to dna damage, which serves to maintain genome integrity. | [in vitro]
previous study found that the proliferation induced by cd40(+) interleukin-21 stimulation could be completely blocked by cc-115, and cd40-mediated resistance to fludarabine and venetoclax could also be reverted by cc-115. moreover, bcr-mediated signaling was blocked by cc-115 and in cll samples from patients with acquired resistance to idelalisib treatment [1]. | [in vivo]
preclinical studies showed that cc-115 had good in vivo pk profiles across multiple species with 53%, 76%, and around100% oral bioavailability in mouse, rat, and dog, respectively [2]. | [target]
| Target | Value | DNA-PK
(Cell-free assay) | 0.013 μM | mTOR
(Cell-free assay) | 0.021 μM | PI3Kα
(Cell-free assay) | 0.852 μM |
| [IC 50]
21/ 13 nm for mtor/dna-pk | [storage]
Store at -20°C | [References]
[1] thijssen r,et al. dual tork/dna-pk inhibition blocks critical signaling pathways in chronic lymphocytic leukemia. blood.2016 jul 28;128(4):574-83.
[2] mortensen ds, et al. optimization of a series of triazole containing mammalian target of rapamycin (mtor) kinase inhibitors and the discovery of cc-115. j med chem. 2015 jul 23;58(14):5599-5608. |
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