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CC-115 FII75TFH5L
Investigational Source: NCT02977780: Phase 2 Interventional Recruiting Glioblastoma (2017)
Source URL: https://clinicaltrials.gov/ct2/show/NCT02977780
CC-115 FII75TFH5L
Investigational Source: NCT02977780: Phase 2 Interventional Recruiting Glioblastoma (2017)
Source URL: https://clinicaltrials.gov/ct2/show/NCT02977780
Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H16N8O |
| Molecular Weight | 336.3512 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI ![Structure of CC-115]( "Structure of CC-115")
SHOW STEREO... HIDE STEREO... SMILES
CCN1C(=O)CNC2=C1N=C(C=N2)C3=C(C)N=C(C=C3)C4=NN=CN4
InChI
InChIKey=GMYLVKUGJMYTFB-UHFFFAOYSA-N InChI=1S/C16H16N8O/c1-3-24-13(25)7-18-15-16(24)22-12(6-17-15)10-4-5-11(21-9(10)2)14-19-8-20-23-14/h4-6,8H,3,7H2,1-2H3,(H,17,18)(H,19,20,23)
HIDE SMILES / InChI DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/27235137
CC-115 is a recently identified inhibitor of the mammalian Target of Rapamycin Kinase (TORK) and DNA-Dependent Protein Kinase (DNA-PK). It is under investigation in phase II clinical trials for the treatment for Glioblastoma and in phase I trials for the treatment of prostate cancer, Ewing's, Osteosarcoma, Chronic Lymphocytic Leukemia and Squamous Cell Carcinoma of the Head and Neck.
Originator
Celgene
15Sources: https://www.ncbi.nlm.nih.gov/pubmed/26102506 Approval Year
Unknown
139594 Targets
Targets
| Primary Target | Pharmacology | Condition | Potency | | Serine/threonine-protein kinase mTOR35Target ID: P42345Gene ID: 2475.0Gene Symbol: MTORTarget Organism: Homo sapiens (Human)Sources: https://www.ncbi.nlm.nih.gov/pubmed/26102506 | Inhibitor8297 | 0.021 µM [IC50] |
| DNA-dependent protein kinase catalytic subunit4Target ID: P78527|||Q9UME3Gene ID: 5591.0Gene Symbol: PRKDCTarget Organism: Homo sapiens (Human)Sources: https://www.ncbi.nlm.nih.gov/pubmed/26102506 | Inhibitor8297 | 0.013 µM [IC50] |
Conditions
Conditions
| Condition | Modality | Targets | Highest Phase | Product | | Chronic lymphocytic leukemia59Sources: https://www.ncbi.nlm.nih.gov/pubmed/27235137 | Primary | Phase I428 | UnknownApproved UseUnknown |
| Prostate cancer178Sources: https://clinicaltrials.gov/show/NCT01353625 | Primary | Phase I428 | UnknownApproved UseUnknown |
Ewing's osteosarcom1Sources: https://clinicaltrials.gov/show/NCT01353625 | Primary | Phase I428 | UnknownApproved UseUnknown |
| Glioblastoma65Sources: https://clinicaltrials.gov/ct2/show/NCT02977780 | Primary | Phase II1132 | UnknownApproved UseUnknown |
Cmax
Cmax
| Value | Dose | Co-administered | Analyte | Population | | 173 ng/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 25 mg 1 times / day single, oraldose: 25 mgroute of administration: Oralexperiment type: SINGLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 162 ng/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 15 mg 2 times / day multiple, oraldose: 15 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 244 ng/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 40 mg 1 times / day multiple, oraldose: 40 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 51.8 ng/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 10 mg 2 times / day multiple, oraldose: 10 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 75.2 ng/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 10 mg 2 times / day multiple, oraldose: 10 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 198 ng/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 25 mg 1 times / day multiple, oraldose: 25 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
AUC
AUC
| Value | Dose | Co-administered | Analyte | Population | | 1716 ng × h/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 25 mg 1 times / day single, oraldose: 25 mgroute of administration: Oralexperiment type: SINGLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 2056 ng × h/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 15 mg 2 times / day multiple, oraldose: 15 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 2650 ng × h/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 40 mg 1 times / day multiple, oraldose: 40 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 622 ng × h/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 10 mg 2 times / day multiple, oraldose: 10 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 66 ng × h/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 10 mg 2 times / day multiple, oraldose: 10 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 1573 ng × h/mLEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 25 mg 1 times / day multiple, oraldose: 25 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
T1/2
T1/2
| Value | Dose | Co-administered | Analyte | Population | | 7.9 hEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 25 mg 1 times / day single, oraldose: 25 mgroute of administration: Oralexperiment type: SINGLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
| 3.98 hEXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31853198 | 10 mg 2 times / day multiple, oraldose: 10 mgroute of administration: Oralexperiment type: MULTIPLEco-administered: | CC-115 plasma | Homo sapienspopulation: UNHEALTHYage: ADULTsex: FEMALE / MALEfood status: FASTED |
Sourcing
Sourcing
| Vendor/Aggregator | ID | URL | | 1PlusChem LLC | 1P000JYN | https://www.1pchem.com/search?query=1P000JYN |
| 1PlusChem LLC | 1P009D1L | https://www.1pchem.com/search?query=1P009D1L |
| AChemBlock | O33758 | http://www.achemblock.com/catalogsearch/result/?q=O33758 |
| ApexBio Technology | B6114 | https://www.apexbt.com/catalogsearch/result/?q=B6114 |
| AstaTech | 44159 | http://astatechinc.com/CPSResult.php?CRNO=44159 |
| BLD Pharm | BD630024 | http://www.bldpharm.com/search/Search.html?keyword=BD630024 |
| BLD Pharm | BD630098 | http://www.bldpharm.com/search/Search.html?keyword=BD630098 |
| Cayman Chemical | 19420 | http://www.caymanchem.com/app/template/Product.vm/catalog/19420 |
| Chem Scene | CS-4561 | http://www.chemscene.com/goproductList/searchProductList?productObj=CS-4561 |
| Chem Scene | CS-5379 | http://www.chemscene.com/goproductList/searchProductList?productObj=CS-5379 |
| ChemShuttle | 140477 | https://www.chemshuttle.com/catalogsearch/result/?q=140477 |
| KeyOrganics | AS-74848 | http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-74848 |
| Lab Network | LN01341555 | https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01341555 |
| MedChem Express | HY-16962 | https://www.medchemexpress.com/search.html?q=HY-16962A&ft=&fa=&fp= |
| MedChem Express | HY-16962A | https://www.medchemexpress.com/search.html?q=HY-16962A&ft=&fa=&fp= |
| MolPort | MolPort-044-183-473 | https://www.molport.com/shop/molecule-link/MolPort-044-183-473 |
| MolPort | MolPort-044-560-393 | https://www.molport.com/shop/molecule-link/MolPort-044-560-393 |
| MolPort | MolPort-046-033-571 | https://www.molport.com/shop/molecule-link/MolPort-046-033-571 |
| MolPort | MolPort-046-417-172 | https://www.molport.com/shop/molecule-link/MolPort-046-417-172 |
| MolPort | MolPort-046-702-084 | https://www.molport.com/shop/molecule-link/MolPort-046-702-084 |
| Molnova | M10883 | https://www.molnova.com/en/serch-list.html?keywords=M10883 |
| Molnova | M11206 | https://www.molnova.com/en/serch-list.html?keywords=M11206 |
| MuseChem | I005747 | https://www.musechem.com/product/I005747.html |
| ShangHai Biochempartner | BCP16702 | http://www.biochempartner.com/search_BCP16702 |
| ShangHai Biochempartner | BCP20709 | http://www.biochempartner.com/search_BCP20709 |
| eMolecules | 106929350 | https://orderbb.emolecules.com/search/#?query=106929350 |
| eMolecules | 208087683 | https://orderbb.emolecules.com/search/#?query=208087683 |
| eMolecules | 222564514 | https://orderbb.emolecules.com/search/#?query=222564514 |
| eMolecules | 75542243 | https://orderbb.emolecules.com/search/#?query=75542243 |
| eMolecules | 89941990 | https://orderbb.emolecules.com/search/#?query=89941990 |
| mcule | MCULE-3559529294 | https://mcule.com/MCULE-3559529294/ |
| mcule | MCULE-6536966585 | https://mcule.com/MCULE-6536966585/ |
PubMed
PubMed
| Title | Date | PubMed | | Reversible thiazolidine exchange: a new reaction suitable for dynamic combinatorial chemistry. | 2009 Aug 6 | 19585999 |
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. | 2015 Jul 23 | 26102506 |
| Dual TORK/DNA-PK inhibition blocks critical signaling pathways in chronic lymphocytic leukemia. | 2016 Jul 28 | 27235137 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/show/NCT01353625 Dose level starts with 0.5mg daily by mouth in cycles of 28 days. Level increases for different patient cohorts in 100% or 50% increments until optimal dose schedule is established for further study. Treatment continues for as long as patient benefits (i.e., until disease progression or unacceptable toxicity).Route of Administration:
Oral In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27235137 To determine whether combined inhibition of TORK and DNA-PK induces cell death, there were compared CC-115 (range of concentration from 0.001 until 10 uM) to inhibitors that are more specific: CC-214, CC-292, idelalisisb, and NU7441. To correct for variability in viability between thawed primary chronic lymphocytic leukemia (CLL) samples, specific apoptosis was calculated. CC-214 (TORKi), CC-292 (BTKi), idelalisib (PI3Kδi), and NU7441 (DNAPKi) induced modest cell death (IC50 > 10 µM and maximum induction of apoptosis at 10 µM of 30-40 %. Whereas CC-115 induced cell death with an IC50 of 0.51 µM. Cell death was due to on-target inhibition of TORK and DNA-PK, because the combination of the TORK inhibitor CC-214 and the DNA-PK inhibitor NU7441 resulted in cell death comparable to CC-115. CC-115 induced cell death in clinically relevant prognostic CLL subgroups.
| Name | Type | Language |
| | Common Name | English |
| | Common Name | English |
| 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-B)PYRAZIN-2(1H)-ONE | Sources: | | Systematic Name | English |
| 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)- | Sources: | | Systematic Name | English |
| 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 | Sources: | | Systematic Name | English |
| Code System | Code | Type | Description |
| | DB12740 Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
| | 300000041470 Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
| | C97040 Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
| | CHEMBL3545426 Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
| | 1228013-15-7 Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
| | FII75TFH5L Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
| | 58298318 Created by admin on Sat Dec 16 08:26:44 GMT 2023 , Edited by admin on Sat Dec 16 08:26:44 GMT 2023 | PRIMARY |
ACTIVE MOIETY FII75TFH5L
CC-115 NIH NCATS PRIVACY ACT ACCESSIBILITY DISCLAIMER HHS VULNERABILITY DISCLOSURE For language access assistance, contact the NCATS Public Information Officer National Center for Advancing Translational Sciences (NCATS), 6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966 version 1.1