2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. FAK ERK Apoptosis
  4. GZD-552

GZD-552 是一种强效的、口服有效的 FAK 抑制剂，对人源 FAK 的 IC50 为 5.8 nM。GZD-552 可抑制 FAK 的磷酸化激活及下游 ERK 信号通路。GZD-552 可诱导细胞凋亡和 G2/M 期细胞周期阻滞，在多形性胶质母细胞瘤细胞中表现出抗增殖活性。GZD-552 在小鼠异种移植模型中表现出抗肿瘤功效。GZD-552 可用于多形性胶质母细胞瘤的相关研究。

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GZD-552

GZD-552 Chemical Structure

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GZD-552 相关抗体

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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

GZD-552 is a potent orally active FAK inhibitor with a human FAK IC50 of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G2/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme[1].

体外研究
(In Vitro)

GZD-552 (compound 16c) 可强效且选择性地抑制 U87-MG 和 U118-MG 胶质母细胞瘤细胞的增殖，其 IC50 值分别为 6.6 nM 和 4.3 nM；同时该化合物对 NCI-H1975 细胞 (IC50 = 0.16 μM)、MDA-MB-231 细胞 (IC50 = 0.28 μM) 和 LO2 细胞 (IC50 = 0.74 μM) 的活性有限[1]。
GZD-552 可在 U87-MG 细胞中与 FAK 蛋白发生强且稳定的结合[1]。
GZD-552 (0.002-0.08 μM) 以浓度依赖的方式抑制 U87-MG 细胞中 FAK 蛋白的表达与激活，并下调下游 ERK 的磷酸化水平[1]。
GZD-552 (0.004-0.12 μM; 24 h) 可在 U87-MG 细胞中诱导剂量依赖性凋亡及 G2/M 期细胞周期阻滞[1]。

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

GZD-552 相关抗体:

Cell Cycle Analysis[1]

Cell Line: U87-MG cells
Concentration: 0.004; 0.04; 0.08; 0.12 μM
Incubation Time: 24 h
Result: Induced apoptosis in U87-MG cells in a concentration manner.
Exhibited early apoptosis rate of 8.99% and the late apoptosis rate of 19% at 0.12 μM.

Apoptosis Analysis[1]

Cell Line: U87-MG cells
Concentration: 0.004; 0.04; 0.08; 0.12 μM
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest in U87-MG cells in a concentration manner.
Increased the proportions of cells in
the G2/M phase to 54.09%, 57.22%, 68.77%, and 71.74%, at 0.004, 0.04, 0.08, and 0.12 μM, respectively.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 AUC0-t AUC0-∞ MRT0-t MRT0-∞ F Vz CL
Mice[1] 2 mg/kg i.v. 1299 ng/mL 0.361 h 461 ng·h/mL 466 ng·h/mL 0.254 h 0.277 h / 2457 mL/kg 4814 mL/h/kg
Mice[1] 10 mg/kg i.g. 467 ng/mL 1.90 h 274 ng·h/mL 279 ng·h/mL 1.07 h 1.25 h 18.7 % / /
体内研究
(In Vivo)

GZD-552 (compound 16c) (10-20 mg/kg，连续 18 天) 可在小鼠 U87-MG 异种移植模型中抑制肿瘤生长，且无可见的全身毒性[1]。

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

Animal Model: Female BALB/c nude mice (5-week-old, 18-22 g) subcutaneously injected with U87-MG cells[1]
Dosage: 10; 20 mg/kg/day
Administration: i.g.; daily; 18 days
Result: Achieved a tumor growth inhibition (TGI) rate of 92.36%.
Achieved a tumor growth inhibition (TGI) rate of 96.68%.
Caused no significant fluctuations in mouse body weight.
Showed no histological abnormalities in heart, liver, spleen, lung, and kidney compared to the control group.
Significantly inhibited FAK, p-FAK, ERK, and p-ERK protein expression in tumor tissues.
分子量

577.55

Formula

C27H30F3N5O6
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-552 相关分类

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  • 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-552GZD552GZD 552FAKERKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseExtracellular signal regulated kinasesG2/M cell cycle arrestERK signalingxenograft modelBALB/c nude mouseU87-MGU118-MGnormal hepatocytesglioblastoma multiforme cellsapoptotic cell deathInhibitorinhibitorinhibit

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