CC-115
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1250 | Check With Us |
| 500mg | $1850 | Check With Us |
| 1g | $2775 | Check With Us |
: Cat #: V2567 CAS #: 1228013-15-7 Purity ≥ 98%
Description: CC-115 (CC115) is a novel and potent dual inhibitor of DNA-PK (DNA-dependent protein kinase) and mTOR (mammalian target of rapamycin) with IC50s of 13 nM and 21 nM, respectively and with potential antineoplastic activity.
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- Related Biological Data
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| Molecular Weight (MW) | 336.35 |
|---|---|
| Molecular Formula | C16H16N8O |
| CAS No. | 1228013-15-7 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 67 mg/mL (199.2 mM)rr |
| Water: <1 mg/mLrr | |
| Ethanol: <1 mg/mL | |
| Synonyms | CC115 ; CC-115; 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 |
| Protocol | In Vitro | CC-115 inhibits PC-3 cells proliferation with an IC50 of 138 nM. In a kinase selectivity assessment against a panel of 250 protein kinases at 3 μM, only one kinase other than mTOR kinase is identified with more than 50% inhibition (cFMS 57%, IC50=2.0 μM).PI3K-alpha (IC50=0.85 μM), ATR (50% inhibition at 30 μM) and ATM (IC50>30 μM). The IC50 values for CC-115 are >10 μM against a panel of CYP enzymes and >33 μM for the hERG (human ether-a-go-go-related gene) ion channel. When screened in a single point assay at 10 μM against a Cerep receptor and enzyme panel only one target is inhibited >50% (PDE3, IC50=0.63 μM);CC-115 proves to be equipotent against DNA PK (IC50=15 nM) and demonstrates 40 to >1000 fold selectivity against the remaining PIKKs teste. |
|---|---|---|
| In Vivo | CC-115 shows good in vivo PK profiles across multiple species with 53%, 76% and ~100% oral bioavailability in mouse, rat and dog, respectively. CC-115 is tested at lower doses of 0.25, 0.5 and 1 mg/kg bid or 1 mg/kg qd, with observed corresponding tumor volume reductions of 46%, 57%, 66% and 57% respectively. CC-115 sustains inhibition though 24 hours. At the 1 mg/kg dose CC-115 shows significant inhibition at 1 and 3 hours, CC-115 demonstrating inhibition through 10 hours. CC-115 is evaluated using both once (qd) and twice (bid) daily dosing schedules |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.9731 mL | 14.8655 mL | 29.7309 mL | 59.4619 mL |
| 5mM | 0.5946 mL | 2.9731 mL | 5.9462 mL | 11.8924 mL |
| 10mM | 0.2973 mL | 1.4865 mL | 2.9731 mL | 5.9462 mL |
| 20mM | 0.1487 mL | 0.7433 mL | 1.4865 mL | 2.9731 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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