1. Protein Tyrosine Kinase/RTK
  2. FAK
  3. Y15

Y15  (Synonyms: FAK Inhibitor 14)

目录号: HY-12444 纯度: ≥98.0%
COA 产品使用指南

Y15是一种有效,特异性的粘着斑激酶抑制剂 (FAK),可抑制其自身磷酸化活性,降低癌细胞的活力,阻断肿瘤生长。

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Y15 Chemical Structure

Y15 Chemical Structure

CAS No. : 4506-66-5

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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 价格 是否有货 数量
5 mg ¥246
In-stock
10 mg ¥400
In-stock
50 mg ¥850
In-stock
100 mg ¥1550
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

IC50 & Target

FAK[1]

体外研究
(In Vitro)

Y15 直接阻断 FAK 的自磷酸化活性。Y15 在 Panc-1 细胞中从 0.1 μM 开始抑制 FAK 的 Y397 磷酸化。在 100 μM 的剂量下,Y15 具有与 TAE226 相同或更好的抑制作用。值得注意的是,总 FAK 在较高剂量的 Y15 下调。Y15 还阻断 FAK 下游底物桩蛋白的磷酸化。在类似于 FAK 的较高剂量下总桩蛋白减少。因此,Y15 以剂量依赖的方式抑制 FAK 磷酸化[1]。MTS 测定是在所有细胞系 (分别为 TT、K1、BCPAP 和 TPC1) 上使用一系列 Y15 剂量完成的。Y15 在所有评估的甲状腺细胞系中以剂量依赖性方式抑制细胞活力。对于 TT、TPC1、BCPAP 和 K1,IC50 值分别为 2.05、5.74、9.99 和 17.54 μM[2]
在用 Y15 处理的巨噬细胞中,丝状伪足和 lamellipodia 保持移动。在用 Y15 处理的细胞中,巨噬细胞周围的颗粒苔藓显得更大[4]

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

体内研究
(In Vivo)

FAKIGF-1R 酪氨酸激酶双重抑制剂 TAE226 处理携带 Panc si-ctrl 肿瘤异种移植裸鼠,为 FAK和IGF-1R 双重抑制的抗肿瘤作用提供参考。在没有药物处理的情况下,Panc si5-IGF-1R 异种移植肿瘤比 Panc si-ctrl 异种移植肿瘤生长慢 (Panc si5-IGF-1R/PBS vs. Panc si-ctrl/PBS),表明仅通过抑制 IGF-1R 通路实现中度肿瘤抑制. Y15 处理对 FAK 活性的进一步抑制更显著地抑制了 Panc si5-IGF-1R 异种移植肿瘤的生长 (Panc si5-IGF-1R/PBS 对比 Panc si5-IGF-1R/ Y15)。在用 TAE226 处理的 Panc si-ctrl 异种移植物中观察到类似的抗肿瘤作用 (Panc si5-IGF-1R/ Y15 对比 Panc si-ctrl/TAE226)。小鼠在整个实验过程中表现出正常的梳理和进食习惯[3]

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

分子量

284.01

Formula

C6H14Cl4N4

CAS 号
性状

固体

颜色

Off-white to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Store at room temperature, keep dry and cool

溶解性数据
细胞实验: 

H2O 中的溶解度 : 50 mg/mL (176.05 mM; 超声助溶 (<50°C))

DMSO 中的溶解度 : 25 mg/mL (88.03 mM; 超声助溶 (<60°C); 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 3.5210 mL 17.6050 mL 35.2100 mL
5 mM 0.7042 mL 3.5210 mL 7.0420 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 10 mg/mL (35.21 mM); 澄清溶液; 超声助溶 (<60°C)

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

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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

参考文献
Kinase Assay
[1]

10 μCi of [γ-32P]-ATP in a kinase buffer 20 mM HEPES, pH 7.4, 5 mM MgCl2, 5 mM MnCl2, 0.1 mM Na3VO4 with 0.1 μg of purified FAK protein are incubated in a kinase buffer with 10 μCi of [γ-32P]-ATP. The kinase reaction is performed for 5 minutes at room temperature and stopped by addition of 2× Laemmli buffer. Proteins are separated on a Ready SDS-10% PAGE gel, and the phosphorylated enolase is visualized by autoradiography[1]

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

Cell Assay
[1]

The cells are treated with Y15 or TAE226 at different concentrations for 24 hours. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium compound from Promega Viability kit is added, and the cells are incubated at 37°C for 1-2 hours. The optical density on 96-plate is analyzed with a microplate reader at 490 nm to determine cell viability. In addition, cells are stained with trypan blue after 24 hours of treatment with Y15 and the percent of cells that stained positive are determined with a hemacytometer[1]

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

Animal Administration
[3]

Mice[3]
Six-week-old, female nude mice are used. 5×106 Panc si5-IGF-1R cells are mixed with matrigel and injected subcutaneously into the flank of athymic nude mice (day 0). Animals are randomly divided into two groups on day 7. One group (n=5) received Y15 (30 mg/kg) and the other received PBS as control treatment (n=5). For Panc si-ctrl xenografts, 5×106 Panc si-ctrl cells are mixed with matrigel and injected subcutaneously into the flank of nude mice. These animals are also randomly divided into two groups on day 7, and one group (n=5) received TAE226 (30 mg/kg), the other group received PBS (n=5) as control treatment. The drugs and PBS are administered through intraperitoneal injection in a total volume of 0.1 mL. Tumor sizes are measured every 3 or 4 d in length (mm)×width (mm) starting from day 10. Tumor volume is calculated as volume (cm3)= 1/2×length (cm)×width(cm)2.

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

参考文献

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 / H2O 1 mM 3.5210 mL 17.6050 mL 35.2100 mL 88.0251 mL
5 mM 0.7042 mL 3.5210 mL 7.0420 mL 17.6050 mL
10 mM 0.3521 mL 1.7605 mL 3.5210 mL 8.8025 mL
15 mM 0.2347 mL 1.1737 mL 2.3473 mL 5.8683 mL
20 mM 0.1761 mL 0.8803 mL 1.7605 mL 4.4013 mL
25 mM 0.1408 mL 0.7042 mL 1.4084 mL 3.5210 mL
30 mM 0.1174 mL 0.5868 mL 1.1737 mL 2.9342 mL
40 mM 0.0880 mL 0.4401 mL 0.8803 mL 2.2006 mL
50 mM 0.0704 mL 0.3521 mL 0.7042 mL 1.7605 mL
60 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.4671 mL
80 mM 0.0440 mL 0.2201 mL 0.4401 mL 1.1003 mL
H2O 100 mM 0.0352 mL 0.1761 mL 0.3521 mL 0.8803 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
Y15
目录号:
HY-12444
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