2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. DNA-PK mTOR
  4. CC-115 hydrochloride

CC-115 hydrochloride 

目录号: HY-16962A 纯度: 98.03%
COA 产品使用指南

摩尔计算器

CC-115 hydrochloride 是一种有效的双重 DNA-PK 和 mTOR 抑制剂，IC50 分别为 13 nM 和 21 nM。CC-115 阻断 mTORC1 和 mTORC2 信号通路。

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CC-115 hydrochloride Chemical Structure

CC-115 hydrochloride Chemical Structure

CAS No. : 1300118-55-1

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥825
In-stock
5 mg ￥750
In-stock
10 mg ￥1200
In-stock
50 mg ￥3840
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of CC-115 hydrochloride:

CC-115 hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 2 篇科研文献

查看 mTOR 亚型特异性产品:

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mTOR mTORC1 mTORC2

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(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].

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

CC-115 hydrochloride 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

372.81

Formula

C16H17ClN8O
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
细胞实验： 

H2O 中的溶解度 : 50 mg/mL (134.12 mM; 超声助溶)

DMSO 中的溶解度 : ≥ 30 mg/mL (80.47 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂： PBS

    Solubility: 100 mg/mL (268.23 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献
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.
参考文献

CC-115 hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / 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
H2O 100 mM 0.0268 mL 0.1341 mL 0.2682 mL 0.6706 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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-1151300118-55-1CC115CC 115DNA-PKmTORDNA-dependent protein kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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