2. GPCR/G Protein Stem Cell/Wnt Apoptosis Cytoskeleton MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. PAK Apoptosis Ras ERK
  4. AZA197

AZA197 是 Cdc42 的选择性小分子抑制剂。AZA197 通过下调 PAK1 和ERK 信号通路，在体外抑制结肠癌细胞增殖、细胞迁移、侵袭，增加细胞凋亡 (apoptosis)。AZA197 抑制肿瘤生长，显著提高 SW620 肿瘤异种移植小鼠存活率。AZA197 可用于结肠癌的研究。

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AZA197

AZA197 Chemical Structure

CAS No. : 1249398-09-1

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1 mg ￥1655
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AZA197 相关抗体

Top Publications Citing Use of Products

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

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K-Ras H-Ras N-Ras Ras

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts. AZA197 can be used for the study of colon cancer[1].

体外研究
(In Vitro)

AZA197 (1-100 μM, 24 h) 促进 SW620 结肠癌细胞中 LDH 释放并抑制 Cdc42 活化[1]。
AZA197 (1-10 μM, 24-72 h) 以剂量和时间依赖性方式显著抑制 SW620 和 HT-29 细胞的增殖[1]。
AZA197 (2-10 μM, 24 h) 诱导 SW620 细胞凋亡并导致细胞周期停滞[1]。
AZA197 (1-5 μM, 24 h) 以剂量依赖性方式显著抑制 SW620 和 HT-29 细胞的迁移和侵袭能力[1]。
AZA197 (2-10 μM, 24 h) 抑制 Cdc42，从而破坏其在 SW620 和 HT-29 细胞中调节细胞形态和运动的关键功能[1]。
AZA197 (2-10 μM, 24 小时) 抑制 Cdc42，从而抑制 SW620 和 HT-29 细胞中下游的 PAK-ERK 信号轴[1]。

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

AZA197 相关抗体:

Apoptosis Analysis[1]

Cell Line: SW620 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: Increased the number of apoptotic cells (sub G0/G1 peak, M1) in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: SW620 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: led to an increase in the proportion of Sub G0/G1 phase and a decrease in the proportions of cells in S phase and G2/M phase.

Cell Migration Assay [1]

Cell Line: SW620 and HT-29 cells
Concentration: 1, 2 and 5 μM
Incubation Time: 24 h
Result: Significantly reduced cancer cell migration by 47.4% and 43.5%, respectively at 2 and 5 μM in SW620 cells.
Significantly reduced cancer cell migration in a dose-dependent manner up to 77.1% in HT-29 colon cancer cells.

Cell Migration Assay [1]

Cell Line: SW620 and HT-29 cells
Concentration: 1, 2 and 5 μM
Incubation Time: 24 h
Result: Significantly decreased SW620 invasion by 61.3%, 71.0% and 83.9%.
Significantly decreased invasion of HT-29 cells at corresponding concentrations up to 84.6%.

Immunofluorescence[1]

Cell Line: SW620 and HT-29 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: Caused the cells to become round, the filamentous pseudopodia to completely disappear, and the actin cytoskeleton to undergo reorganization.

Western Blot Analysis[1]

Cell Line: SW620 and HT-29 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: Significantly and dose-dependently reduced the levels of phosphorylated PAK (p-PAK) and phosphorylated ERK (p-ERK).
Did not affect the protein expression levels of Cdc42, total PAK, and total ERK.
Significantly reduced the protein expression level of Cyclin D1.
体内研究
(In Vivo)

MSC778 (100 μg，溶于100 μL 30% DMSO (HY-Y0320C)，腹腔注射，每天一次，持续 2 周或 100 天) 在结肠癌异种移植模型中显著抑制了肿瘤生长，显著延长了荷瘤小鼠的生存期[1]。

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

Animal Model: SW620 xenograft model established in Balb/c nude, female mice[1]
Dosage: 100 μg, dissolved in 100 μL of 30% DMSO
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks or 100 days
Result: Significantly inhibited tumor growth.
Significantly prolonged the survival period of tumor-bearing mice.
Inhibited the proliferation of tumor cells and induced cell apoptosis within the body.
Reduced the levels of p-PAK and p-ERK in the tumor tissue.
分子量

408.58

Formula

C24H36N6
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 4.5 mg/mL (11.01 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4475 mL 12.2375 mL 24.4750 mL
5 mM 0.4895 mL 2.4475 mL 4.8950 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。-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。

  • 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
纯度 & 产品资料
参考文献

AZA197 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。-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 1 mM 2.4475 mL 12.2375 mL 24.4750 mL 61.1875 mL
5 mM 0.4895 mL 2.4475 mL 4.8950 mL 12.2375 mL
10 mM 0.2448 mL 1.2238 mL 2.4475 mL 6.1188 mL
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:

AZA1971249398-09-1AZA 197AZA-197PAKApoptosisRasERKp21 activated kinasesExtracellular signal regulated kinasesCdc42 InhibitorXenograft modelColon cancerInhibitorinhibitorinhibit

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目录号：
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