2. Protein Tyrosine Kinase/RTK
  3. FAK
  4. FAK-IN-26

FAK-IN-26 是一种可穿透血脑屏障的 Focal Adhesion Kinase (FAK) 抑制剂 (IC50：0.87 nM)。FAK-IN-26 显著抑制 A549 和 SKOV-3 细胞系中的肿瘤细胞活力、癌症干细胞活性和细胞迁移。FAK-IN-26 具有强效抗癌活性，在 A549 和 SKOV-3 肿瘤小鼠模型中，其抑瘤率分别为 59.15% 和 57.9%。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

FAK-IN-26 Chemical Structure

FAK-IN-26 Chemical Structure

CAS No. : 2801785-12-4

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

FAK-IN-26 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 %[1].

IC50 & Target

0.87 nM
体外研究
(In Vitro)

FAK-IN-26 (Compound A8) 对 FAK 具有优异的结合能力，Kd 值为 15 μM[1]。
FAK-IN-26 (1 μmol/L) 对多种激酶具有广谱抑制活性，其中对 FAK 和 FYNα 的抑制率超过 95%[1]。
FAK-IN-26 (0.5-10 μM) 与 Defactinib (VS6063) (HY-12289) 相比，其在较低浓度下即可显著降低 A549 和 SKOV-3 细胞的活力。 FAK-IN-26 (0.2-1.6 μM) 剂量依赖性减少 A549 和 SKOV-3 细胞中的癌症干细胞群[1]。
FAK-IN-26 (62.5-1000 nM，72 小时) 显著诱导 A549 和 SKOV-3 细胞系的 G2/M 期停滞[1]。
FAK-IN-26 (0.1-10 nM，6-48 小时) 剂量依赖性地降低 A549 和 SKOV-3 细胞的迁移率和距离，在 1 nM 和 10 nM 浓度下均观察到显著抑制作用[1]。
FAK-IN-26 (31.25-62.5 nM，48 小时) 以剂量依赖性方式有效抑制 A549 和 SKOV-3 细胞系中的 FAK 自身磷酸化，且在 A549 细胞中的抑制作用更佳[1]。
FAK-IN-26 在人肝微粒体中具有良好的代谢稳定性，CLint 和 T1/2 分别为 31.8 μL/min/mg 和 43.6 分钟[1]。

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

FAK-IN-26 相关抗体:

Cell Cycle Analysis[1]

Cell Line: A549 cells, SKOV-3 cells
Concentration: 62.5, 125, 250, 500, 1000 nM
Incubation Time: 72 h
Result: Significantly arrested A549 cells and SKOV-3 cells in the G2/M phase, and the proportion of A549 cells were 70.8 %, 68.7 %, 68.8 %, 57.9 %, and 44.7 %, respectively.

Cell Migration Assay [1]

Cell Line: A549 cells, SKOV-3 cells
Concentration: 0.1, 1, 10 nM
Incubation Time: 6, 12, 24, 48 h
Result: Dose-dependently decreased migration rates and distances of A549 and SKOV-3 cells with significant inhibition observed at concentrations of 1 nM and 10 nM.

Western Blot Analysis[1]

Cell Line: A549 cells, SKOV-3 cells
Concentration: 31.25, 62.5 nM
Incubation Time: 48 h
Result: Effectively inhibited the protein expression of p-FAK925 in both A549 and SKOV-3 cells in a dose-dependent manner, with greater efficacy in A549 cells.
体内研究
(In Vivo)

FAK-IN-26 (Compound A8) (25-50 mg/kg，口服，每日一次或两次，连用 5 天，然后停药 2 天，共 28 天) 在 A549 和 SKOV-3 肿瘤小鼠模型中均比 Defactinib (VS6063) (HY-12289)、Erlotinib (HY-50896) 和 Paclitaxel (HY-B0015) 具有更强的抗肿瘤作用，并且与 Paclitaxel 联合用药可进一步增强 SKOV-3 肿瘤模型中的疗效[1]。
FAK-IN-26 (500-2000 mg/kg) 在小鼠中耐受性良好，最高剂量可达 2000 mg/kg，且不会引起急性毒性[1]。
FAK-IN-26 具有良好的肿瘤摄取和保留性，在 S180 肿瘤小鼠中注射 30 分钟后，峰值摄取量为 4.16 ID/g，并有效穿透 BBB，在 15 分钟时脑摄取量为 2.63 % ID/g，在 120 分钟时为 1.62 % ID/g[1]。

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

Animal Model: Kunming mice were injected subcutaneously with A549 and KOV-3 cells until tumor volume reached 70-100 mm3[1].
Dosage: A549 tumor model: 50 mg/kg, SKOV-3 tumor model: 25 mg/kg
Administration: oral gavage (p.o.), once a day for five days followed by two days off (A549 tumor model), twice daily for five days followed by two days off (SKOV-3 tumor model), and then measures tumor volume and weight.
Result: Significantly increased tumor inhibition rate of 59.15 %, superior to VS6063 and Erlotinib with tumor inhibition rate of 40.69 % and 47.41 % in the A549 tumor model.
Achieved tumor inhibition rate of 57.9 %, superior to VS6063 and Paclitaxel with tumor inhibition rate of 53.89 % and 55.30 %, and the combination therapy with Paclitaxel further enhanced anti-tumor effects (tumor inhibition rate: 76.63 %) in the SKOV-3 tumor model.
分子量

460.30

Formula

C20H19BrFN5O2
CAS 号
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-26 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-262801785-12-4FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseFAK inhibitorsLung cancerOvarian cancerA549 cellsKOV-3 cellsInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
FAK-IN-26
目录号：
HY-173515
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z