CC-115

Name: CC-115
Brand: MedChemExpress
SKU: HY-16962
Rating: 5.0 (2 reviews)

Cat. No.: HY-16962 Pureza: 99.10%: Ficha de datos
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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

CC-115 Estructura química

No. CAS : 1228013-15-7

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 2 publication(s) in Google Scholar

Other Forms of CC-115:

CC-115 hydrochloride In-stock

2 Publications Citing Use of MCE CC-115

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas mTOR:

Ver todas las isoformas

mTOR mTORC1 mTORC2

Actividad biológica
Protocolo
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

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.

IC₅₀ & Target^[1]

DNA-PK

13 nM (IC₅₀)

mTOR

21 nM (IC₅₀)

mTORC1

mTORC2

PI3Kα

852 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	0.138 3 Compound: 26	Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs	[PMID: 26102506]
PC-3	IC₅₀	0.022 3 Compound: 26	Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr	[PMID: 26102506]
PC-3	IC₅₀	0.023 3 Compound: 26	Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr	[PMID: 26102506]
PC-3	IC₅₀	0.023 3 Compound: 26	Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr	[PMID: 26102506]
PC-3	IC₅₀	0.022 3 Compound: 26	Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr	[PMID: 26102506]
PC-3	IC₅₀	0.138 3 Compound: 26	Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs	[PMID: 26102506]
PC-3	IC₅₀	0.022 3 Compound: 26	Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr	[PMID: 26102506]
PC-3	IC₅₀	0.023 3 Compound: 26	Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr	[PMID: 26102506]
PC-3	IC₅₀	0.138 3 Compound: 26	Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs	[PMID: 26102506]

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 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.

Ensayo clínico

Peso molecular

336.35

Fòrmula

C₁₆H₁₆N₈O

No. CAS

1228013-15-7

Appearance

Solid

SMILES

O=C1CN=C2C(N1CC)=NC(C3=C(C)N=C(C4=NN=CN4)C=C3)=CN2

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (297.31 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9731 mL	14.8655 mL	29.7309 mL
5 mM	0.5946 mL	2.9731 mL	5.9462 mL
10 mM	0.2973 mL	1.4865 mL	2.9731 mL

View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad
Calculadora de dilución

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.10%

Select Batch:

Ficha de datos (279 KB) SDS (394 KB)

COA (248 KB) HNMR (142 KB) RP-HPLC (163 KB) LCMS (106 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Ensayo de quinasas ^[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Ensayo celular ^[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales ^[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9731 mL	14.8655 mL	29.7309 mL	74.3273 mL
	5 mM	0.5946 mL	2.9731 mL	5.9462 mL	14.8655 mL
	10 mM	0.2973 mL	1.4865 mL	2.9731 mL	7.4327 mL
	15 mM	0.1982 mL	0.9910 mL	1.9821 mL	4.9552 mL
	20 mM	0.1487 mL	0.7433 mL	1.4865 mL	3.7164 mL
	25 mM	0.1189 mL	0.5946 mL	1.1892 mL	2.9731 mL
	30 mM	0.0991 mL	0.4955 mL	0.9910 mL	2.4776 mL
	40 mM	0.0743 mL	0.3716 mL	0.7433 mL	1.8582 mL
	50 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4865 mL
	60 mM	0.0496 mL	0.2478 mL	0.4955 mL	1.2388 mL
	80 mM	0.0372 mL	0.1858 mL	0.3716 mL	0.9291 mL
	100 mM	0.0297 mL	0.1487 mL	0.2973 mL	0.7433 mL

CC-115 Related Classifications

Help & FAQs

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-1151228013-15-7CC115CC 115DNA-PKmTORDNA-dependent protein kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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CC-115

Revisión del cliente

Other Forms of CC-115:

CC-115 Related Antibodies

2 Publications Citing Use of MCE CC-115

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas mTOR:

Actividad biológica

Protocolo

Pureza y Documentación

Referencias

Revisión del cliente

CC-115 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

CC-115 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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