2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. VEGFR-2-IN-80

VEGFR-2-IN-80 是一种 VEGFR-2 抑制剂，其 IC50 为 2.206 μM。VEGFR-2-IN-80 可与 VEGFR-2 的 ATP 结合残基相互作用，从而抑制其激酶活性。VEGFR-2-IN-80 可抑制毛细血管样网络的形成，对多种人类癌细胞产生细胞毒性作用，并可抑制 HCT116 异种移植物的生长。VEGFR-2-IN-80 可用于结直肠癌的相关研究。

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VEGFR-2-IN-80

VEGFR-2-IN-80 Chemical Structure

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VEGFR-2-IN-80 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-80 is a VEGFR-2 inhibitor with an IC50 of 2.206 μM. VEGFR-2-IN-80 interacts with ATP-binding residues of VEGFR-2 to inhibit its kinase activity. VEGFR-2-IN-80 suppresses formation of capillary-like networks, exerts cytotoxic effects against various human cancer cells, and suppresses growth of HCT116 xenografts. VEGFR-2-IN-80 can be used for the research of colorectal cancer[1].

IC50 & Target

VEGFR2

2.206 μM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-80 (SA7) (2 μM；作用 30 分钟) 可在人脐静脉内皮细胞 (HUVEC) 中抑制 VEGFR-2，其 IC50 为 2.206 μM[1]。
VEGFR-2-IN-80 (6.25-200 μM；72 小时) 对人类癌细胞系 (SKOV3、HT29、HCT116 等) 表现出广谱细胞毒性，IC50 值处于低微摩尔级别，且在非癌细胞 HEK293 中的活性较低[1]。
VEGFR-2-IN-80 (无细胞毒性浓度；预孵育 30 分钟，基质胶孵育 16 小时) 可抑制人脐静脉内皮细胞 (HUVEC) 中毛细血管样网络的形成，在无细胞毒性浓度下抑制率为 44.89%[1]。

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

VEGFR-2-IN-80 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: SKOV3, HT29, HCT116, DU145, 22Rv1, A549, MCF7, Mel P, SK-MEL28, SW620, HEK293
Concentration: 6.25-200 μM
Incubation Time: 72 h
Result: Exhibited low-micromolar cytotoxicity across various cancer cell lines, with IC50 values of 5.6 μM (SKOV3), 9.3 μM (HT29), 11.3 μM (HCT116), 14.5 μM (DU145), 16.6 μM (22Rv1), 15.7 μM (A549), 15.4 μM (MCF7), 13.4 μM (Mel P), 11.4 μM (SK-MEL28), and 13.6 μM (SW620); showed reduced activity in HEK293 cells with an IC50 of 46.8 μM.
体内研究
(In Vivo)

VEGFR-2-IN-80 (SA7) (25-50 mg/kg；灌胃；每日给药；连续 21 天) 在 HCT116 异种移植瘤小鼠中呈现剂量依赖性抗肿瘤功效，其中 50 mg/kg 剂量组的肿瘤生长抑制率达 65.5%[1]。

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

Animal Model: BALB/c nude mice (male, 6-8 weeks old, 22 ± 2 g, HCT116 xenograft model)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced average tumor volume to 1690 mm3 (TGI 47%) versus control at 25 mg/kg; reduced average tumor volume to 1094 mm3 (TGI 65.5%) versus control at 50 mg/kg.
分子量

534.51

Formula

C27H17F3N4O3S
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-80 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)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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-80VEGFRVascular endothelial growth factor receptorcolorectal cancerHEK293 cellsHUVEC cellsHT29ATP-binding residueskinase activitySKOV3VEGFR-2HCT116 xenograftshuman cancer cellsInhibitorinhibitorinhibit

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