2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. VEGFR-2-IN-43

VEGFR-2-IN-43 (compound 16) 是一种具有口服活性的 VEGFR2 抑制剂，IC50 为 39.91 μM。VEGFR-2-IN-43 可用于湿性年龄相关性黄斑变性 (w-AMD) 疾病研究。

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VEGFR-2-IN-43 Chemical Structure

VEGFR-2-IN-43 Chemical Structure

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VEGFR-2-IN-43 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-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research[1].

IC50 & Target[1]

VEGFR2

39.91 μM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-43 (compound 16) (0-50 μM, 72 h) 对 LX-2 细胞的增殖具有弱抑制作用，对BaF3-Tel-VEGFR2 细胞的增值具有明显抑制作用[1]。
VEGFR-2-IN-43 (0-10 μM, 48 h) 对 HUVEC 细胞中的 VEGFR2 磷酸化表现出浓度依赖性抑制[1]。
VEGFR-2-IN-43 (1 μM, 0-120 min) 表现出显著的血浆稳定性和中等的肝微粒体稳定性[1]。

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

VEGFR-2-IN-43 相关抗体:

Cell Proliferation Assay[1]

Cell Line: BaF3-Tel-VEGFR2 cells, BaF3 cells (BaF3-Tel-VEGFR2 cells were constructed through viral transgene technology using BaF3 cells as a template, and their proliferation was dependent on VEGFR2 kinase.)
Concentration: 0-50 μM
Incubation Time: 72 h
Result: The GI50 value of VEGFR-2-IN-43 (compound 16) for BAF3-tel-VEGFR2 cells was 22.9 nM, and the proliferation of BaF3 cells was almost not inhibited.
体内研究
(In Vivo)

VEGFR-2-IN-43 (compound 16) (2/10 mg/kg, i.v. and p.o.) 在 ICR mice 中表现出可接受的口服生物利用度 (F = 20.2%)[1]。

药代动力学分析[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT0-t (h) Cmax (ng/mL) Tmax (h) T1/2 (h) F (%)
i.v. 2 508 512 0.665 853 0.0833 1.32 /
p.o. 10 506 518 0.72 321 0.417 1.58 20.2

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

470.49

Formula

C24H27FN4O5
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-43 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 *
= × ×

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)
× = ×
C1   V1   C2   V2
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-43VEGFRVascular endothelial growth factor receptorLX-2 cellsHUVEC cellsWater solubilityICR micew-AMDOral administrationBaF3-TEL-VEGFR2 cellsHergCardiac safetyliver microsomal stabilityplasma stabilityHalf timeInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-163403
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