CC-115 Hydrochloride | DNA-PK/mTOR Inhibitor - MedChemExpress
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- CC-115 hydrochloride
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CC-115 hydrochloride 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.
For research use only. We do not sell to patients.
CC-115 hydrochloride Chemical Structure
CAS No. : 1300118-55-1
| Size | Price | Stock | |
|---|---|---|---|
| Solution | |||
| 10 mM * 1 mL in DMSO | Ask For Quote & Lead Time | ||
| Solid | |||
| 5 mg | Ask For Quote & Lead Time | ||
| 10 mg | Ask For Quote & Lead Time | ||
| 25 mg | Ask For Quote & Lead Time | ||
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Other In-stock Forms of CC-115 hydrochloride:
CC-115Other Forms of CC-115 hydrochloride:
- CC-115 In-stock
CC-115 hydrochloride Related Antibodies
2 Publications Citing Use of MCE CC-115 hydrochloride
- •Sci Data. 2024 Sep 19;11(1):1024.
- •Front Pharmacol. 2020 Nov 11;11:580407. [Abstract]
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View All Isoforms mTOR mTORC1 mTORC2Biological Activity
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Customer Review
| Description | CC-115 hydrochloride 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. | |||||
|---|---|---|---|---|---|---|
| IC50 & Target[1] |
| |||||
| 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). Of the PI3K related kinases (PIKKs) tested, CC-115 proves to be equipotent against DNA PK (IC50=15 nM) and demonstrates 40 to >1000 fold selectivity against the remaining PIKKs tested; 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)[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. CC-115 hydrochloride Related Antibodies | |||||
| In Vivo | CC-115 hydrochloride 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[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||
| Clinical Trial | ||||||
| Molecular Weight | 372.81 | |||||
| Formula | C16H17ClN8O | |||||
| CAS No. | 1300118-55-1 | |||||
| Appearance | Solid | |||||
| Color | Light yellow to yellow | |||||
| SMILES | [H]Cl.O=C1CN=C2C(N1CC)=NC(C3=C(C)N=C(C4=NN=CN4)C=C3)=CN2 | |||||
| Shipping | Room temperature in continental US; may vary elsewhere. | |||||
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | |||||
| Purity & Documentation | Data Sheet (276 KB) SDS (251 KB) Handling Instructions (2659 KB) | |||||
| References |
|
| Kinase Assay [1] | An HTR-FRET substrate phosphorylation assay is employed for mTOR kinase. PI3Kα IC50 determinations are outsourced using the mobility shift assay format. Compounds (e.g., CC-115) are assessed against concentrations of ATP at approximately the Km for the assay, with average ATP Km of 15 μM and 50 μM for the mTOR and PI3K assays, respectively[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
|---|---|
| Cell Assay [1] | PC-3 cells are cultured in growth media. For biomarker studies cells are treated for 1 h and then assayed for pS6 and pAkt levels using MesoScale technology. For proliferation experiments, cells are treated with compound (e.g., CC-115) and then allowed to grow for 72 h. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as IC50 values[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Animal Administration [1] | Mice[1] Encouraged by the observed exposures, CC-115 is advanced into single dose PK/PD studies assessing mTOR pathway biomarker inhibition in tumor bearing mice. PC-3 tumor-bearing mice are administered with a single dose of CC-115, dosed orally at either 1 or 10 mg/kg, and plasma and tumor samples are collected at various time points for analysis. Significant inhibition of both mTORC1 (pS6) and mTORC2 (pAktS473) is observed for all compounds and the level of biomarker inhibition correlated to plasma compound levels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| References |
|
-
[1]. 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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CC-115 hydrochloride Related Classifications
- Disease Areas
- Cancer Neurological, Eye or Ear Disease Blood or Cardiovascular Disease Metabolic or Endocrine Disease Respiratory Disease Digestive System Disease Urogenital Disease
- Blood Disease Lipid Metabolism Pulmonary Disease Lung Cancer Breast Cancer Colorectal Cancer Digestive System Cancer Prostate Cancer Urogenital Cancer Gastric Cancer Liver Cancer Leukemia/Lymphoma/Myeloma Pancreatic Cancer Ovarian Cancer Pain
- Leukemia/Lymphoma/Myeloma Obesity Lung Fibrosis
- Cancer
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- Cell Cycle/DNA Damage PI3K/Akt/mTOR
- DNA-PK mTOR
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| kg g mg μg ng pg | = | M mM μM nM pM | × | L mL μL | × |
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
| Concentration (start) | × | Volume (start) | = | Concentration (final) | × | Volume (final) |
|---|---|---|---|---|---|---|
| M mM μM nM pM | × | L mL μL | = | M mM μM nM pM | × | L mL μL |
| C1 | V1 | C2 | V2 |
- Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
CC-1151300118-55-1CC115CC 115DNA-PKmTORDNA-dependent protein kinaseMammalian target of RapamycinInhibitorinhibitorinhibit
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