CC-115 hydrochloride

Name: CC-115 hydrochloride
Brand: MedChemExpress
SKU: HY-16962A
Rating: 5.0 (1 reviews)

Cat. No.: HY-16962A Purity: 98.23%: FAQs
Data Sheet SDS COA Handling Instructions

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	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of CC-115 hydrochloride:

CC-115 In-stock

1 Publications Citing Use of MCE CC-115 hydrochloride

•Front Pharmacol. 2020 Nov 11;11:580407. [Abstract]

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mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
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]

DNA-PK

13 nM (IC₅₀)

mTOR

21 nM (IC₅₀)

mTORC1

mTORC2

PI3Kα

852 nM (IC₅₀)

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.

Clinical Trial

Molecular Weight

372.81

Appearance

Solid

Formula

C₁₆H₁₇ClN₈O

CAS No.

1300118-55-1

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)

Solvent & Solubility

In Vitro:

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

DMSO : ≥ 30 mg/mL (80.47 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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.

In Vivo:

1.

Add each solvent one by one: PBS
Solubility: 100 mg/mL (268.23 mM); Clear solution; Need ultrasonic

*All of the co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 98.23%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (249 KB) RP-HPLC (216 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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. [Content Brief]