1. Metabolic Enzyme/Protease Apoptosis
  2. Ser/Thr Kinase Apoptosis
  3. CQ3196

CQ3196 是一种口服 RIOK2 抑制剂,Kd 值为 14 nM。CQ3196 能有效抑制 RIOK2 的 ATPase 活性,IC50 值为 72 nM。CQ3196 抑制胃癌细胞系的细胞增殖和集落形成,诱导 HGC-27 和 AGS 细胞凋亡 (apoptosis)。CQ3196 抑制 RIOK2 的下游信号通路,降低 mTORAKT 磷酸化,并且调节核糖体功能和蛋白质合成。CQ3196 抑制肿瘤生长,可用于胃癌的体内外研究。

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CQ3196

CQ3196 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CQ3196 is an orally active RIOK2 inhibitor with a Kd of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC50 value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research[1].

体外研究
(In Vitro)

CQ3196 (72 小时) 可抑制多种癌细胞的增殖,IC50 分别为 0.46 μM (HGC-27)、0.73 μM (AGS)、2.34 μM (KATO III)、2.09 μM (PC-9)、1.56 μM (A549)、1.42 μM (H3255)、0.75 μM (Mia paca-2)、1.75 μM (Hela)、1.46 μM (Molt 4)、0.90 μM (K562) 和 1.52 μM (HEK-293)[1]
CQ3196 (30-1000 nM,14 天) 在300 nM 及以上浓度下可完全抑制 HGC-27 和 AGS 细胞中的集落形成[1]
CQ3196 (30-1000 nM,48 小时) 以浓度依赖性方式诱导 HGC-27 和 AGS 细胞早期和晚期凋亡[1]
CQ3196 (30-1000 nM) 显著降低 HGC-27 细胞中 mTORAKT 的磷酸化[1]
CQ3196 (30-1000 nM,48 小时) 可降低核糖体小亚基 RPS2 的表达[1]
CQ3196 (1 μM,24 小时) 可下调 RPS、RPL 和一些核糖体相关蛋白,从而调节核糖体功能和蛋白质合成[1]

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

Apoptosis Analysis[1]

Cell Line: HGC-27 and AGS cells
Concentration: 30, 100, 300, and 1000 nM
Incubation Time: 48 h
Result: Induced apoptosis in HGC-27 cells in a concentration-dependent manner, with the apoptotic rate increasing from 6.31 % to 21.12 % at 1000 nM.
Induced apoptosis in AGS cells, with apoptotic cell levels increasing from 6.74 % to 18.2 % at 1000 nM.

Western Blot Analysis[1]

Cell Line: HGC-27 cells
Concentration: 30, 100, 300, and 1000 nM
Incubation Time: 48 h
Result: Decreased ribosomal small subunit RPS2 expression.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 10 mg/kg p.o. AUC0-t 3.5*10^3 μg/L·h
Rat 2 mg/kg i.v. AUC0-t 3.0*10^3 μg/L·h
Rat 10 mg/kg p.o. Cmax 169 ng/mL
Rat 2 mg/kg i.v. T1/2 19.1 h
Rat 10 mg/kg p.o. F 23.4 %
Rat 2 mg/kg i.v. Cmax 559 ng/mL
Rat 2 mg/kg i.v. CL 403 mL/h/kg
体内研究
(In Vivo)

CQ3196 (25 和 50 mg/kg,口服,每两天一次,持续 12 天) 在 BALB/c 裸鼠建立的 HGC-27 胃癌异种移植模型中表现出剂量依赖性抗肿瘤作用[1]

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

Animal Model: Male Balb/c-Nude (6 weeks old) injected subcutaneously with HGC-27 cells[1]
Dosage: 25 and 50 mg/kg
Administration: p.o., every two days for 12 days
Result: Inhibited tumor growth, with Tumor Growth Inhibition (TGI) of 43.0 % (25 mg/ kg) and 62.3 % (50 mg/kg).
Revealed no significant body weight loss in mice.
分子量

577.60

Formula

C30H30F3N7O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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

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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.

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产品名称:
CQ3196
目录号:
HY-175733
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