2. Protein Tyrosine Kinase/RTK Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. FAK Apoptosis Reactive Oxygen Species (ROS) Caspase
  4. FAK-IN-28

FAK-IN-28 是具有口服活性的 FAK 抑制剂 (IC50 = 0.4 nM)。FAK-IN-28 具有双重抗增殖和抗转移功效。FAK-IN-28 通过 ROS 升高触发 caspase-3 依赖性细胞凋亡 (apoptosis)。FAK-IN-28 抑制肿瘤生长，且不会引起体重减轻或肝肾毒性。FAK-IN-28 可用于 FAK 驱动的恶性肿瘤的研究，例如结肠癌、宫颈癌、三阴性乳腺癌和黑色素瘤。

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FAK-IN-28

FAK-IN-28 Chemical Structure

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3.  试用装只面向终端客户。

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FAK-IN-28 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FAK-IN-28 is an orally active FAK inhibitor (IC50 = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma[1].

IC50 & Target[1]

Caspase 3

 

体外研究
(In Vitro)

FAK-IN-28 (Compound 10c) (12 小时) 对 HCT116、HeLa、MDA-MB-231 和 A375 细胞表现出细胞毒作用，IC50 分别为 0.08、0.31、0.23 和 0.29 μM[1]。
FAK-IN-28 (0.2-25 μM，1-24 小时) 可抑制 HCT116 细胞侵袭，并减少 HCT116 细胞中的粘附细胞数量[1]。
FAK-IN-28 (0.2-25 μM，12-24 小时) 可增强 caspase-3 活化，增加凋亡细胞数量，并扰乱 HCT116 细胞的细胞周期进程[1]。
FAK-IN-28 (1-125 μM，12 小时) 在 HCT116 细胞中表现出 ROS 诱导活性[1]。

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

FAK-IN-28 相关抗体:

Cell Migration Assay [1]

Cell Line: HCT116 cells
Concentration: 0.2 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 12 h, 24 h
Result: Inhibited cell invasion at 0.5 μM and enhanced inhibition at 2 μM, which was superior to TAE226 (HY-13203) at the same concentration.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 25 μM
Incubation Time: 12 h, 24 h
Result: Enhanced caspase-3 activation and the number of apoptotic cell populations.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.2 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Increased G2/M cells and decreased the G0/G1 cell population.
体内研究
(In Vivo)

FAK-IN-28 (Compound 10c) (50 mg/kg，口服，每日一次，10 天) 在 HCT116 异种移植裸鼠模型中可抑制肿瘤生长，并且不引起明显的体重减轻或肝肾毒性[1]。

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

Animal Model: HCT116 (5 × 106) xenograft female Balb/c nude mice model[1]
Dosage: 50 mg/kg
Administration: p.o., once daily, 10 days
Result: Inhibited tumor growth by 62.22% (TAE226 group was 50.98%).
Did not change body weight, kept serum biochemical parameters (ALT, AST, ALP, LDH) within normal range, and did not cause pathological changes (necrosis, inflammation or fibrosis).
分子量

795.83

Formula

C37H40F3N9O6S
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

FAK-IN-28 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

FAK-IN-28FAKApoptosisReactive Oxygen Species (ROS)CaspasePTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorHCT116 cellsHCT116 xenograftNude miceinhibitorinhibit

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