2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK Immunology/Inflammation NF-κB Apoptosis
  3. Carbonic Anhydrase VEGFR Reactive Oxygen Species MDM-2/p53 Bcl-2 Family Cytochrome P450 Caspase
  4. CA IX/VEGFR-2-IN-2

CA IX/VEGFR-2-IN-2 (compound 5e) 是一种双靶向抑制剂。CA IX/VEGFR-2-IN-2 对 CA IX (KI=3.1 μM) 和 VEGFR-2 (IC50=32.1 nM) 均有较强的抑制作用。CA IX/VEGFR-2-IN-2 可用于胰腺癌 (PANC1)， 乳腺癌 (MCF7) 和前列腺癌细胞 (PC3) 的研究。

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CA IX/VEGFR-2-IN-2 Chemical Structure

CA IX/VEGFR-2-IN-2 Chemical Structure

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CA IX/VEGFR-2-IN-2 相关抗体

Top Publications Citing Use of Products

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CA CA I CA Ⅱ CA Ⅸ CA XII

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) [1].

IC50 & Target[1]

VEGFR-2

32.1 nM (IC50)

CA Ⅸ

3.1 μM (Ki)

体外研究
(In Vitro)

CA IX/VEGFR-2-IN-2 (compound 5e) 对反应性肿瘤细胞的选择性顺序是 PANC1，其次是 MCF7 和 PC3 并降低了 PANC1 细胞的迁移[1]。
CA IX/VEGFR-2-IN-2 (compound 5e) 在胰腺癌细胞中诱导了 p53，BAX，细胞色素 C 和 caspases 3，8，9 表达的上调以及 Bcl-2 基因表达的下调引起细胞凋亡[1]。
CA IX/VEGFR-2-IN-2 (compound 5e) 抑制 HIF-1α 表达从 6.1±0.13 ng/mL 降低到 3.7±0.09 ng/mL，抑制幅度超过 1.5 倍在 PANC1 细胞中[1]。
CA IX/VEGFR-2-IN-2 (compound 5e) 引起 ROS 形成异常增加导致 PANC1 细胞周期停止或凋亡在 PANC1 细胞中[1]。

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

CA IX/VEGFR-2-IN-2 相关抗体:

Cell Proliferation Assay[1]

Cell Line: PANC1 , MCF7 and PC3 cell lines
Concentration:
Incubation Time:
Result: Had a better growthinhibition effect on PANC1 and MCF7 cell lines, with IC50 values of 1.04 μM and 1.40 μM, had lower inhibitory effects against PC3, with an IC50 greater than 5 μM.

Cell Cycle Analysis[1]

Cell Line: PANC1 cell lines
Concentration:
Incubation Time: 24 h
Result: Increased the early apoptosis ratio from 0.37% (DMSO) to 21.39%, as did the late apoptosis ratio from 0.18 → 11.11.
体内研究
(In Vivo)

CA IX/VEGFR-2-IN-2 (compound 5e) (5 和 10 mg/kg，腹腔注射，持续两周) 在雌性瑞士白化小鼠体内减少肿瘤体积和重量方面比标准药物 DOX (10 mg/kg) 更有效[1]。
CA IX/VEGFR-2-IN-2 (compound 5e) (5 和 10 mg/kg，腹腔注射，持续两周) 对雌性瑞士白化小鼠注射 10 mg/kg 导致 VEGF， MMP-2 和 MMP-9 浓度的进一步降低[1]。
CA IX/VEGFR-2-IN-2 (compound 5e) (5 和 10 mg/kg，腹腔注射，持续两周) 对雌性瑞士白化小鼠注射 5 mg/kg 导致坏死区域的形成， 并散布着不同的肿瘤细胞， 而在 10 mg/kg 的剂量下则有明显的改善， 肌肉束中的弥散性和广泛性坏死区域被取代， 肿瘤细胞的数量明显减少， 表明对活的肿瘤细胞有实质性的抑制[1]。

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

Animal Model: solid Ehrlich carcinoma (SEC)
Dosage: 5 and 10 mg/kg
Administration:
Result: Led to a 47.28% decrease in tumor volume and a 55.42% decrease in tumor weight at a dose of 5 mg/kg compared to the solid Ehrlich carcinoma.
Led to a 65.88% reduction in the volume of the tumor and a 75.71% decrease in tumor weight at a dose of 10 mg/kg relative to the control group of SEC.
分子量

423.46

Formula

C22H18FN3O3S
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

CA IX/VEGFR-2-IN-2 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:

CA IX/VEGFR-2-IN-2Carbonic AnhydraseVEGFRReactive Oxygen SpeciesMDM-2/p53Bcl-2 FamilyCytochrome P450CaspaseCarbonate dehydrataseVascular endothelial growth factor receptorCYPsDouble-targeted inhibitorPANC1 MCF7 and PC3 cell linessolid Ehrlich carcinomaInhibitorinhibitorinhibit

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