2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway Apoptosis JAK/STAT Signaling
  3. VEGFR ERK Apoptosis EGFR
  4. AGW-11

AGW-11 是一种强效的双重抑制剂，能够抑制 EGFR (IC50 = 556 nM) 和 VEGFR2 (IC50 = 289.7 nM)。AGW-11 可诱导凋亡 (apoptosis)，并抑制 HUVECs 中 EGFR、VEGFR2 和 ERK1/2 的磷酸化。AGW-11 有效抑制癌细胞生长，减少 HUVEC 的增殖、管腔形成和侵袭，从而阻断血管生成。AGW-11 在 4T1 异种移植小鼠模型中显著抑制肿瘤生长并减少肺转移。AGW-11 可用于乳腺癌的研究。

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AGW-11

AGW-11 Chemical Structure

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AGW-11 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 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer[1].

IC50 & Target[1]

VEGFR2

289.7 nM (IC50)

EGFR

556 nM (IC50)

体外研究
(In Vitro)

AGW-11 (0.5-30 μM，48 h) 在 MDA-MB-231、4T1、A2780 和 HCT-116 癌细胞中表现出显著的抗增殖活性，IC50 值分别为 1.26 μM、2.85 μM、0.75 μM 和 1.58 μM[1]。
AGW-11 (0.5-2 μM，24 h) 以浓度依赖性方式显著抑制 MDA-MB-231 细胞中 EGFR 和 ERK1/2 的磷酸化[1]。
AGW-11 (2 μM，24 h) 强效抑制 4T1 乳腺癌细胞的集落形成，并诱导 apoptosis[1]。
AGW-11 (1-4 μM，6-24 h) 强效抑制 HUVEC 的管腔形成，并对 HUVEC 侵袭表现出浓度依赖性的抑制作用[1]。
AGW-11 (1-4 μM，24 h) 在 HUVECs 中以浓度依赖性方式有效降低 VEGFR2 和 ERK1/2 的磷酸化[1]。

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

AGW-11 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1. 2 μM
Incubation Time: 24 h
Result: Inhibited the phosphorylation of EGFR and ERK1/2 in MDA-MB-231 cells in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: 4T1 breast cancer cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Induced apoptosis in 4T1 breast cancer cells.
体内研究
(In Vivo)

AGW-11 (1-5 mg/kg，腹腔注射，每隔一天一次，持续 20 天) 在 BALB/c 小鼠 4T1 乳腺癌异种移植模型中表现出显著的抗肿瘤活性[1]。

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

Animal Model: 4T1 mouse breast cancer cells (1×106 cells per mouse) were subcutaneously inoculated into the dorsal region of 4-6-week-old female BALB/c mice (18-20 g body weight)[1]
Dosage: 1 mg/kg and 5 mg/kg
Administration: i.p., once every 2 days, 20 days
Result: Achieved tumor volume reduction rates of 34.5% and 32.4% at doses of 1 mg/kg and 5 mg/kg.
Showed no significant changes in body weight.
Reduced the Ki67 expression and reduced the CD31 and VEGF expressions.
Decreased the phosphorylation of VEGFR2 and its downstream molecule ERK1/2.
Increased the level of cleaved caspase 3.
Reduced the number of metastatic lung nodules.
Enhanced tumor necrosis and inhibited abnormal transformation of liver and lung tissues.
分子量

532.63

Formula

C31H36N2O6
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

AGW-11 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:

AGW-11AGW11AGW 11VEGFRERKApoptosisEGFRVascular endothelial growth factor receptorExtracellular signal regulated kinasesEpidermal growth factor receptorErbB-1HER1breast cancerVEGFR2HUVECs,4T1 cellsInhibitorinhibitorinhibit

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