CC-115 hydrochloride|cas:1300118-55-1|西域试剂

CC-115 hydrochloride,98.23%

产品编号：Bellancom-16962A| CAS NO：1300118-55-1| 分子式：C₁₆H₁₇ClN₈O| 分子量：372.81

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货号	价格	库存与货期
Bellancom-16962A	￥900.00	杭州北京（现货）
Bellancom-16962A	￥1500.00	杭州北京（现货）
Bellancom-16962A	￥5200.00	杭州北京（现货）

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CC-115 hydrochloride

产品介绍

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。

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.

体外研究

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).

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

体内研究

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.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

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

DMSO : ≥ 30 mg/mL (80.47 mM)

* "≥" 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
10 mM	0.2682 mL	1.3412 mL	2.6823 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；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