- CC-115
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- $1.00 / 1ASSAYS
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2019-09-06
- CAS:1228013-15-7
- Min. Order: 1ASSAYS
- Purity: 95%~99%
- Supply Ability: per week:100kg
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| Product Name: | CC-115 | | Synonyms: | 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;CC-115;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]- | | CAS: | 1228013-15-7 | | MF: | C16H16N8O | | MW: | 336.35 | | EINECS: | | | Product Categories: | | | Mol File: | 1228013-15-7.mol |  |
| | CC-115 Chemical Properties |
| 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 |
| | CC-115 Usage And Synthesis |
| Uses | CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling. | | 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 | | 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. |
| | CC-115 Preparation Products And Raw materials |
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