2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis
  3. VEGFR Akt Caspase Bcl-2 Family Apoptosis
  4. VEGFR-2/AKT-IN-2

VEGFR-2/AKT-IN-2 (Compound 5) 是一个 VEGFR-2/AKT 抑制剂 (对人肝肿瘤细胞上VEGFR的 IC50 为 0.061 μM)。VEGFR-2/AKT-IN-2 减少细胞中总的和磷酸化AKT，上调 BAX 和 caspase-3，下调 Bcl-2，从而促进细胞凋亡 (Apoptosis)。VEGFR-2/AKT-IN-2使细胞周期在 S 期停止。VEGFR-2/AKT-IN-2 抑制人肝肿瘤细胞生长。

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VEGFR-2/AKT-IN-2 Chemical Structure

VEGFR-2/AKT-IN-2 Chemical Structure

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VEGFR-2/AKT-IN-2 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

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells[1].

IC50 & Target[1]

VEGFR2

0.061 μM (IC50)

Bcl-2

 

Caspase 3

 

体外研究
(In Vitro)

VEGFR-2/AKT-IN-2 具有与索拉非尼 (HY-10201) 相似的 VEGFR2 抑制活性，IC50 为 0.061 μM[1]。
VEGFR-2/AKT-IN-2 (0.39-100 μM, 48 h) 抑制 HepG-2 和 HuH-7 细胞系生长，其 IC50 值分别为 0.75 和 3.43 μM[1]。
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) 减少 HepG-2 细胞中总的和磷酸化的 AKT[1]。
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) 促进细胞凋亡，增加早期和晚期凋亡细胞占比 (分别从0.39%增加到26.28%，从0.21%增加到18.87%)，上调 BAX 和 caspase-3，下调 Bcl-2[1]。
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) 阻止 HepG-2 细胞在 S 期的细胞周期进展[1]。

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

VEGFR-2/AKT-IN-2 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG-2, HuH-7, THLE-2
Concentration: 100 μM, 25 μM, 6.25 μM, 1.56 μM, and 0.39 μM.
Incubation Time: 48 h
Result: Inhibited the growth of HepG-2 and HuH-7 cell lines with IC50 of 0.75 μM and 3.43 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: HepG-2
Concentration: 0.75 μM
Incubation Time: 48 h
Result: The cell cycle progression was arrested during the S phase in 48.02% of HepG-2 cells compared to untreated HepG-2 cells (29.66%).
Significantly decreased the proportion of cells in the G2/M phase (58.71%) and increased the proportion of cells in the S phase after 24 h.
分子量

437.49

Formula

C25H16FN5S
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/AKT-IN-2 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/AKT-IN-2VEGFRAktCaspaseBcl-2 FamilyApoptosisVascular endothelial growth factor receptorPKBProtein kinase BHCCHepG-2 cellsHuH-7 cellsCell cycleAnticancerCytotoxicityProliferationInhibitorinhibitorinhibit

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