1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis
  2. VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis
  3. Multi-kinase-IN-2

Multi-kinase-IN-2 (compound 7h) 是一种口服有效的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 对血管激酶包括 VEGFR-1/2/3, PDGFRα/βFGFR-1,以及 LYNc-KIT 激酶表现出极好的抑制活性。Multi-kinase-IN-2 显著减弱 AKTERK 蛋白的磷酸化。Multi-kinase-IN-2 诱导细胞凋亡 (apoptosis)。Multi-kinase-IN-2 显示抗癌活性。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Multi-kinase-IN-2 Chemical Structure

Multi-kinase-IN-2 Chemical Structure

CAS No. : 2095628-21-8

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看 PDGFR 亚型特异性产品:

查看 FGFR 亚型特异性产品:

查看 Akt 亚型特异性产品:

查看 Src 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity[1].

IC50 & Target

VEGFR-3

6.3 ± 0.5 nM (IC50)

VEGFR-2

6.5 ± 0.9 nM (IC50)

VEGFR-1

31 ± 2.1 nM (IC50)

PDGFRα

7.0 ± 0.1 nM (IC50)

PDGFRβ

9.9 ± 0.7 nM (IC50)

FGFR1

23 ± 2.5 nM (IC50)

体外研究
(In Vitro)

Multi-kinase-IN-2 (compound 7h) (0-10 μM, 14 days) potently inhibits colony formation of HT-29, MKN74, and HepG2 cancer cells[1].
Multi-kinase-IN-2 (0-3 μM, 24 h) significantly attenuates phosphorylation of AKT and ERK proteins[1].
Multi-kinase-IN-2 (0-3 μM, 72 h) induces apoptosis of HT-29, MKN74, and HepG2 cell[1].

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

Cell Proliferation Assay[1]

Cell Line: HT-29, HepG2, and MKN74 cells
Concentration: 0, 0.2, 0.5, 1, and 2 μM or 0, 0.3, 1, 3, and 10 μM
Incubation Time: 14 days
Result: Exhibited excellent activity in inhibition of colony formations in a dose-dependent manner, with remarkable activity at 1 µM concentration.

Western Blot Analysis[1]

Cell Line: HT-29 and HepG2
Concentration: 0, 0.2, 0.5, 1, and 2 μM or 0, 0.3, 1, 3, and 10 μM
Incubation Time: 24 h
Result: Suppressed the phosphorylation of AKT (Ser473) in a dose-dependent manner with a significant inhibition of ERK (Thr202/Tyr204) phosphorylation at 3 μM.

Apoptosis Analysis[1]

Cell Line: HT-29, MKN74, and HepG2 cells
Concentration: 0, 0.3, 1, and 3 μM
Incubation Time: 72 h
Result: Triggered severe apoptosis of HT-29, MKN74, and HepG2 cells in a dose-dependent manner.
体内研究
(In Vivo)

Multi-kinase-IN-2 (compound 7h) (100 mg/kg, Orally, once daily for 18 days) displays mild inhibition of tumor growth in mice[1].

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

Animal Model: Female nu/nu mice (4-6 weeks old, HT-29 human colon cancer xenograft model)[1]
Dosage: 100 mg/kg
Administration: Orally, once daily for 18 days
Result: Displayed mild inhibition of tumor growth, with tumor growth inhibition (TGI) value of 13.39%.
分子量

561.67

Formula

C34H35N5O3

CAS 号
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
  • 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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
Multi-kinase-IN-2
目录号:
HY-150026
需求量: