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CC-115 hydrochloride

产品编号 T61505Cas号 1300118-55-1

CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR kinase, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively blocks both mTORC1 and mTORC2 signaling pathways.

CC-115 hydrochloride

CC-115 hydrochloride

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产品编号 T61505Cas号 1300118-55-1

CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR kinase, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively blocks both mTORC1 and mTORC2 signaling pathways.

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500 mg¥ 15,6791-2周
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产品介绍

生物活性
产品描述
CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR kinase, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively blocks both mTORC1 and mTORC2 signaling pathways.
体外活性
CC-115 inhibits PC-3 cells proliferation with an IC 50 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%, IC 50 =2.0 μM). Of the PI3K related kinases (PIKKs) tested, CC-115 proves to be equipotent against DNA PK (IC 50 =15 nM) and demonstrates 40 to >1000 fold selectivity against the remaining PIKKs tested; PI3K-alpha (IC 50 =0.85 μM), ATR (50% inhibition at 30 μM) and ATM (IC 50 >30 μM). The IC 50 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, IC 50 =0.63 μM) [1].
体内活性
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].
化学信息
分子量372.82
分子式C16H17ClN8O
CAS No.1300118-55-1
储存&溶解度
存储Shipping with blue ice.

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多
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