2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FAK Pyk2 Apoptosis
  4. GZD-257

GZD-257 是一种可穿透血脑屏障的 ATP 竞争性 FAK 抑制剂 (IC50 = 14.3 nM)，其对 FAK 的选择性比 Pyk2 高 4.77 倍 (IC50 = 68.2 nM)。GZD-257 可显著诱导 U118MG 细胞凋亡 (apoptosis)，并将细胞周期阻滞于 G2/M 期。GZD-257 可用于胶质母细胞瘤 (GBM) 的研究。

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GZD-257

GZD-257 Chemical Structure

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GZD-257 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

GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM)[1].

体外研究
(In Vitro)

GZD-257 (Compound 7) 对胶质瘤细胞系 U118-MG (IC50 = 1.64 μM) 和 U87-MG (IC50 = 1.40 μM) 表现出强效活性，但对 LO2 细胞的活性较低 (IC50 = 9.35 μM)[1]。
GZD-257 (10 μM，16 h) 的渗透系数 (Pe) 为 43.85× 10-6 cm/s，表明其具有优异的血脑屏障穿透能力[1]。
GZD-257 (1-20 μM，24 h) 以浓度依赖的方式诱导 U118-MG 细胞发生晚期凋亡[1]。
GZD-257 (1-20 μM) 可导致 U118-MG 细胞 G2/M 期阻滞，阻滞比例从 10.38 % 增加至 67.19 %[1]。

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

GZD-257 相关抗体:

Apoptosis Analysis[1]

Cell Line: U118-MG cells
Concentration: 1 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 24 h
Result: Induces late apoptosis in a concentration-dependent manner: 8.42 % at 1 μM, 9.65 % at 5 μM, 11.6 % at 10 μM, and 36.8 % at 20 μM.
分子量

525.00

Formula

C26H29ClN6O4
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

GZD-257 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:

GZD-257GZD257GZD 257FAKPyk2ApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2DesignmGlioblastomaMacrocyclizationInhibitorinhibitorinhibit

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产品名称：
GZD-257
目录号：
HY-178969
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