2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR-IN-13

FGFR-IN-13 (compound III-30) 通过抑制关键蛋白的表达调节内源性 FGFR1(IC50=0.20±0.02 nM) 和 FGFR4(IC50=0.40±0.03 nM) 介导的信号通路。FGFR-IN-13 能够抑制 total-PARP 和 Bcl-2 蛋白的表达，促进 Cleaved-PARP 和 Bax 蛋白的表达，且呈剂量依赖性。FGFR-IN-13 具有显著的抗肿瘤活性且具有口服活性。

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

FGFR-IN-13 Chemical Structure

FGFR-IN-13 Chemical Structure

CAS No. : 2962941-25-7

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

FGFR-IN-13 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

查看所有亚型
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity[1].

体外研究
(In Vitro)

FGFR-IN-13 (10 μM, 9 h) 可以和 FGFR 蛋白实现共价不可逆结合，其抑制 p-FGFR 蛋白表达的能力可以达到 AZD4547(HY-13330) 和 TAS-120(HY-100818) 的水平在 MDA-MB-231 细胞系中[1]。
FGFR-IN-13 (2.5, 5, 10 μM, 24 h) 能呈剂量依赖性诱导细胞凋亡， 在相同浓度 (5 μM) 下诱导凋亡能力优于AZD4547 (45.4% 和 37.3%)， 可能具有与 AZD4547 相似的作用机制，但 MDAMB-231 细胞对 III-30 更为敏感[1]。 FGFR-IN-13 (1.25, 2.5, 5 μM, 12 h) 在不产生明显细胞毒性的剂量下，能有效抑制MDA-MB-231细胞的迁移，且呈剂量依赖性[1]。 FGFR-IN-13 (2.5, 5, 10 μM, 12 h) 能够通过产生过量的ROS和降低MMP来诱导细胞凋亡[1]。

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

FGFR-IN-13 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 9 h
Result: Inhibited the autophosphorylation of FGFR protein for a long period of time, and the expression level of p-FGFR protein in cancer cells is still suppressed even after 8 h of discontinuation.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 μM, 5 μM and 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, and the percentage of induced apoptosis reached 56.8 % at 10 μM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB- 435, MDA-MB-231, KYSE-150, HepG2 and HUVEC cells
Concentration:
Incubation Time: 72 h
Result: Showed better inhibitory effect on KYSE-150 cells (IC50 = 1.93 μM) compared with 2 positive controls.
体内研究
(In Vivo)

FGFR-IN-13 (10 和 30 mg/kg， 每天口服一次持续 21 天) 抑制肿瘤生长呈剂量依赖性，且具有良好的安全性，在安全剂量下可有效抑制肿瘤生长在 MDA-MB-231 异种移植瘤小鼠模型[1]。

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

Animal Model: MDA-MB-231 xenograft tumor mouse model[1]
Dosage: 10 and 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Did not cause significant weight loss.
Achieved tumor growth inhibition (TGI) of 64.21% at high doses (30 mg/kg).
Achieved tumor growth inhibition (TGI) of 40.22% at low doses (10 mg/kg).
分子量

415.44

Formula

C23H21N5O3
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

FGFR-IN-13 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:

FGFR-IN-132962941-25-7FGFRFibroblast growth factor receptorFGFR inhibitorIrreversible covalent inhibitorAnti-tumor activityMDA-MB-231 xenograft tumor mouse modelInhibitorinhibitorinhibit

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：
FGFR-IN-13
目录号：
HY-163527
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z