2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. VEGFR-2-IN-85

VEGFR-2-IN-85 是 VEGFR-2 的强效抑制剂，其 IC50 值为 0.23 μM。VEGFR-2-IN-85 对多种癌细胞系表现出强效的细胞毒性，而对正常细胞的毒性极低。VEGFR-2-IN-85 还可能通过调节 VEGFR-2/p-Akt 通路实现对癌细胞迁移的抑制。VEGFR-2-IN-85 可通过调节 Caspase-3、Bax 和 Bcl-2 诱导细胞凋亡 (apoptosis)。VEGFR-2-IN-85 可将细胞周期阻滞在 G2/M 期，并具有抗血管生成活性。VEGFR-2-IN-85 是一种靶向放射增敏剂，可增强放射诱导的细胞毒性。 VEGFR-2-IN-85 可用于非小细胞肺癌、乳腺癌和肝癌等癌症的研究。

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VEGFR-2-IN-85

VEGFR-2-IN-85 Chemical Structure

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Customer Review

VEGFR-2-IN-85 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-85 is a strong VEGFR-2 inhibitor, with an IC50 value of 0.23 μM. VEGFR-2-IN-85 exhibits potent cytotoxic activity against multiple cancer cell lines with minimal toxicity toward normal cells. VEGFR-2-IN-85 also impairs cancer cell migration, likely through modulation of the VEGFR-2/p-Akt pathway. VEGFR-2-IN-85 can induce apoptosis through modulation of Caspase-3, Bax and Bcl-2. VEGFR-2-IN-85 arrests cell cycle at the G2/M phase and has anti-angiogenic activity. VEGFR-2-IN-85 is a targeted radiosensitizer enhancing radiation-induced cytotoxicity. VEGFR-2-IN-85 can be used for research on cancers such as non-small cell lung cancer, breast cancer, and liver cancer[1].

IC50 & Target[1]

VEGFR-2

0.23 μM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-85 (compound 9a) (48 小时) 在 A549、MDA-MB-231、HepG-2、WI-38 和 MCF10A 细胞系中的 IC50 值分别为 5.02 μM、4.78 μM、4.13 μM、95.87 μM 和 62.95 μM[1]。
VEGFR-2-IN-85 (4.13 μM；48 小时) 可有效干扰 HepG-2 细胞中与血管生成信号相关的细胞迁移[1]。
VEGFR-2-IN-85 (4.13 μM；24 小时) 可降低 HepG-2 细胞中 p-Akt 的表达，证实了 VEGFR-2 介导的信号传导受到抑制[1]。
VEGFR-2-IN-85 (4.13 μM；48 小时) 可显著调节 HepG-2 细胞中的凋亡相关标志物，主要表现为 caspase-3 激活、Bax 上调和 Bcl-2 抑制[1]。
VEGFR-2-IN-85 (4.13 μM；24 小时) 可干扰 HepG-2 细胞的 G2/M 期细胞周期进程，阻止有丝分裂完成并限制细胞增殖[1]。
VEGFR-2-IN-85 (48 小时) 能有效增强 γ 射线对恶性细胞的细胞毒性，同时对正常细胞的影响较小，在 A549 细胞中的 IC50 值为2.10 μM，在 MDA-MB-231 细胞中的 IC50 值为1.89 μM，在 HepG-2 细胞中的 IC50 值为 1.75 μM，在 WI-38 细胞中的 IC50 为 68.74 μM [1]。

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

VEGFR-2-IN-85 相关抗体:

Cell Migration Assay [1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 48 h
Result: Limited wound closure to 56.30%, compared with 97.04% in control group.

Western Blot Analysis[1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 24 h
Result: Decreased p-Akt level compared with control cells, indicating effective suppression of Akt phosphorylation.

Apoptosis Analysis[1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 48 h
Result: Upregulated the expression of Caspase-3 and Bax.
Suppressed the expression of Bcl-2.

Cell Cycle Analysis[1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 24 h
Result: Increased the proportion of G2/M cells from 1.35% in untreated controls to 9.57%.
Decreased the G0/G1 population from 87.14% to 78.13%.
Slightly elevated the S phase fraction (12.21% vs. 11.84% in control).
分子量

574.60

Formula

C25H23FN4O7S2
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-85 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)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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-85VEGFRVascular endothelial growth factor receptorVEGFR-2 inhibitorcytotoxic activityVEGFR-2/p-Akt pathwayapoptosisarrest cell cycletargeted radiosensitizernon-small cell lung cancerbreast cancerliver cancerInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-182745
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