2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. VEGFR Microtubule/Tubulin Apoptosis
  4. VEGFR-2-IN-71

VEGFR-2-IN-71 是 VEGFR2/微管蛋白 (tubulin) 双重抑制剂。VEGFR-2-IN-71 抑制肿瘤细胞增殖并诱导细胞凋亡 (apoptosis) 和细胞周期阻滞。VEGFR-2-IN-71 抑制了鸡胚绒毛尿囊膜 (CAM) 模型中的血管生成。VEGFR-2-IN-71 通过抑制 VEGFR2 和微管蛋白 (tubulin) 抑制 HGC-27 异种移植模型中的肿瘤生长。VEGFR-2-IN-71 在大鼠中口服生物利用度低。VEGFR-2-IN-71 可以用于癌症研究。

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VEGFR-2-IN-71

VEGFR-2-IN-71 Chemical Structure

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VEGFR-2-IN-71 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VEGFR-2-IN-71 is a dual VEGFR2/tubulin inhibitor. VEGFR-2-IN-71 inhibits tumor cell proliferation and induces apoptosis and cell cycle arrest. VEGFR-2-IN-71 inhibits angiogenesis in the chick chorioallantoic membrane (CAM) model. VEGFR-2-IN-71 inhibits tumor growth in the HGC-27 xenograft model by inhibiting VEGFR2 and tubulin. VEGFR-2-IN-71 has low oral bioavailability in rats. VEGFR-2-IN-71 can be used in cancer research[1].

体外研究
(In Vitro)

VEGFR-2-IN-71 (Compound 6r) (1-128 μM，48 小时) 对 HepG-2、HCT-116、HGC-27、MDA-MB-231、MCF-7、HA-VSMC 和 GES-1 细胞均表现出抗肿瘤活性和细胞毒性，IC50 分别为 13.3 μM、18.8 μM、11.4 μM、21.8 μM、17.4 μM、17.1 μM 和 16.73 μM[1]。

VEGFR-2-IN-71 (0-2 μM，24-72 小时) 对 HGC-27 和 HepG-2 细胞表现出抗增殖作用，在 1.0 μM 时达到完全抑制[1]。

VEGFR-2-IN-71 (0-1 μM，10 days) 抑制 HGC-27 和 HepG-2 细胞集落形成[1]。

VEGFR-2-IN-71 (0-1 μM) 在 HGC-27 细胞中通过下调 VEGF 表达和调节糖酵解相关酶 HK2、PFKM 和 PKM2 来抑制 VEGFR2 活性并发挥抗肿瘤作用[1]。

VEGFR-2-IN-71 (0-1 μM) 可抑制 HGC-27 和 HepG-2 细胞中的微管蛋白聚合并破坏微管动力学[1]。

VEGFR-2-IN-71 (0-1 μM) 可诱导 HGC-27 细胞的细胞周期停滞和凋亡[1]。

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

VEGFR-2-IN-71 相关抗体:

Western Blot Analysis[1]

Cell Line: HGC-27 cells
Concentration: 0 μM, 0.25 μM, 0.5 μM , 1 μM
Incubation Time: /
Result: Reduced VEGF protein expression.
Inhibited hexokinase 2 (HK2), phosphofructokinase muscle (PFKM) and pyruvate kinase M2 (PKM2) protein expression.

Apoptosis Analysis[1]

Cell Line: HGC-27 cells
Concentration: 0 μM, 0.25 μM, 0.5 μM , 1 μM
Incubation Time: /
Result: Induced cell cycle arrest at the G2/M phase and apoptosis, with the percentages of apoptotic cells at 0.25, 0.5, and 1 μM were 10.01%, 13.45%, and 16.54%, respectively.
体内研究
(In Vivo)

VEGFR-2-IN-71 (Compound 6r) (1-10 μM，48 小时) 可抑制 CAM 模型中的血管形成[1]。

VEGFR-2-IN-71 (15-30 mg/kg，腹腔注射，隔日一次，共 16 天) 在携带 HGC-27 异种移植瘤的 BALB/c 裸鼠中发挥抗肿瘤活性和血管生成抑制作用[1]。

VEGFR-2-IN-71 (20-100 mg/kg，腹腔注射，每日一次，共 12 天) 不会损害心脏、肝脏、脾脏、肺脏或肾脏，不会造成死亡，表现出良好的安全性[1]。

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

Animal Model: BALB/c nude mice (15-18 g, 5 weeks old) bearing HGC-27 xenografts model (4 × 106 cells subcutaneously implanted in the left armpit) [1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: i.p., every other day, 16 days
Result: Inhibited tumor growth at 15 mg/kg, reduced the growth rates and final weights of tumors, showing an inhibitory effect on tumor growth, with the rates reaching 68.35% at 30 mg/kg.
Reduced the expression of Ki67 and MVD and inhibited angiogenesis within tumors.
Reduced the levels of VEGFA, a marker of angiogenesis, and VEGFR-2, an early marker of endothelial progenitor cells, in tumors.
分子量

532.44

Formula

C26H20F4N2O6
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

VEGFR-2-IN-71 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

VEGFR-2-IN-71VEGFRMicrotubule/TubulinApoptosisVascular endothelial growth factor receptornhibitorHGC-27 cellsBALB/c nude miceAnti-cancerInhibitorinhibitorinhibit

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