Art. -Nr.: HY-16962A

CC-115 hydrochloride

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

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.

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Reinheit: 98.01%
CAS. Nr.: 1300118-55-1
Formel: C₁₆H₁₇ClN₈O
Molecular Weight:372.81

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

CC-115 hydrochloride Chemical Structure

CAS. Nr.: 1300118-55-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

DNA-PK

13 nM (IC₅₀)

mTOR

21 nM (IC₅₀)

mTORC1

mTORC2

PI3Kα

852 nM (IC₅₀)

Alle mTOR Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 1300118-55-1
Appearance Solid
Molecular Weight 372.81
Formel C₁₆H₁₇ClN₈O
Color Light yellow to yellow
SMILES

[H]Cl.O=C1CN=C2C(N1CC)=NC(C3=C(C)N=C(C4=NN=CN4)C=C3)=CN2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (3)

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Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
Tulane University

2026.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 50 mg/mL (134.12 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6823 mL

13.4117 mL

26.8233 mL

5 mM

0.5365 mL

2.6823 mL

5.3647 mL

10 mM

0.2682 mL

1.3412 mL

2.6823 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (268.23 mM); Clear solution; Need ultrasonic

Protokoll

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].

MedChemExpress (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].

MedChemExpress (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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	2.6823 mL	13.4117 mL	26.8233 mL	67.0583 mL
	5 mM	0.5365 mL	2.6823 mL	5.3647 mL	13.4117 mL
	10 mM	0.2682 mL	1.3412 mL	2.6823 mL	6.7058 mL
	15 mM	0.1788 mL	0.8941 mL	1.7882 mL	4.4706 mL
	20 mM	0.1341 mL	0.6706 mL	1.3412 mL	3.3529 mL
	25 mM	0.1073 mL	0.5365 mL	1.0729 mL	2.6823 mL
	30 mM	0.0894 mL	0.4471 mL	0.8941 mL	2.2353 mL
	40 mM	0.0671 mL	0.3353 mL	0.6706 mL	1.6765 mL
	50 mM	0.0536 mL	0.2682 mL	0.5365 mL	1.3412 mL
	60 mM	0.0447 mL	0.2235 mL	0.4471 mL	1.1176 mL
	80 mM	0.0335 mL	0.1676 mL	0.3353 mL	0.8382 mL
	100 mM	0.0268 mL	0.1341 mL	0.2682 mL	0.6706 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

CC-115 hydrochloride

3 Cited Publications

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CC-115 hydrochloride

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Publications Citing Use of MedChemExpress (MCE) CC-115 hydrochloride

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CC-115 hydrochloride Related Classifications

HY-16962A Related Classifications