CC-115 (hydrochloride)
- Product Name
- CC-115 (hydrochloride)
- CAS No.
- 1300118-55-1
- Chemical Name
- CC-115 (hydrochloride)
- Synonyms
- CC-115 HCl;CC-115 (hydrochloride)
- CBNumber
- CB03067002
- Molecular Formula
- C16H17ClN8O
- Formula Weight
- 372.82
- MOL File
- 1300118-55-1.mol
CC-115 (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 30 mg/mL (80.47 mM)
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-5379
- Product name
- CC-115(hydrochloride)
- Purity
- 97.22%
- Packaging
- 5mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-5379
- Product name
- CC-115(hydrochloride)
- Purity
- 97.22%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- orb611858
- Product name
- CC-115 hydrochloride
- Purity
- >98%
- Packaging
- 10mg
- Price
- $402.9
- Updated
- 2021/12/16
- Product number
- CS-5379
- Product name
- CC-115(hydrochloride)
- Purity
- 97.22%
- Packaging
- 50mg
- Price
- $520
- Updated
- 2021/12/16
- Product number
- orb611858
- Product name
- CC-115 hydrochloride
- Purity
- >98%
- Packaging
- 50mg
- Price
- $793.9
- Updated
- 2021/12/16
CC-115 (hydrochloride) Chemical Properties,Usage,Production
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.
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].
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].
Uses
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.
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].
IC 50
DNA-PK: 13 nM (IC50); mTOR: 21 nM (IC50); mTORC1; mTORC2; PI3Kα: 852 nM (IC50)
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.
CC-115 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
CC-115 (hydrochloride) Suppliers
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