2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  3. Cytochrome P450 FGFR
  4. FGFR2/3-IN-3

FGFR2/3-IN-3 是一种双靶点 FGFR2/3 抑制剂，IC50 分别为 2.7 nM (TEL-FGFR2) 和 3.9 nM (TEL-FGFR3)，对野生型和突变型 FGFR3 均具有有效活性。FGFR2/3-IN-3 对 CYP3A4 抑制作用和 hERG 毒性较低。FGFR2/3-IN-3 通过抑制突变型 FGFR3 介导的信号通路，改善软骨细胞增殖与分化失衡，促进骨骼生长。FGFR2/3-IN-3 在侏儒症小鼠模型中显示出促生长作用，具备治疗软骨发育不全 (ACH) 等骨发育障碍相关疾病的潜力。

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

FGFR2/3-IN-3 Chemical Structure

FGFR2/3-IN-3 Chemical Structure

CAS No. : 3069945-78-1

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

FGFR2/3-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to treat bone development disorder-related diseases such as achondroplasia (ACH)[1].

IC50 & Target

CYP2C9

3.9 μM (IC50)

CYP2D6

5.0 μM (IC50)

CYP3A4M

7.2 μM (IC50)

FGFR3

3.9 nM (IC50)

FGFR2

2.7 nM (IC50)

体外研究
(In Vitro)

FGFR2/3-IN-3 (compound 23) 对 FGFR3 野生型 (IC50 = 3.2 nM) 和 V555M 突变型 (IC50 = 0.5 nM) 均表现出强抑制活性，对TEL-FGFR1 (IC50 = 29.4 nM) 和TEL-FGFR4 (IC50 = 29 nM)[1]。

FGFR2/3-IN-3 对 TEL-FGFR3 突变体 Ba/F3 细胞系中常见的 FGFR3G380R (IC50 = 7.0 nM)、FGFR3WT (IC50 = 3.9 nM)、FGFR3V555L (IC50 = 1.7 nM)、FGFR3L608V (IC50 = 10.0 nM) ACH 突变表现出抑制活性[1]。

FGFR2/3-IN-3 抑制 FGFR3 驱动的肿瘤细胞中 RT-112/84 细胞的生长 (IC50 = 1.3 nM)[1]。

FGFR2/3-IN-3 对 CYP 亚型 2C9 (IC50 = 3.9 μM) 和 2D6 (IC50 = 5.0 μM) 的抑制活性略强于对 3A4 亚型的抑制活性[1]。

FGFR2/3-IN-3 (compound 23) (0.2 μM, 1 μM) 可挽救 FGF 诱导的小鼠离体股骨培养模型中的生长迟缓[1]。

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

FGFR2/3-IN-3 相关抗体:
体内研究
(In Vivo)

FGFR2/3-IN-3 (0.5 mg/kg, 2 mg/kg，皮下注射，14 天) 可增强 Fgfr3Y367C/+ 小鼠 ACH 模型中的整体生长，并促进尾部、胫骨和股骨的生长[1]。

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

Animal Model: Fgfr3Y367C/+ mouse model of ACH[1]
Dosage: 0.5 mg/kg, 2 mg/kg
Administration: s.c., 14 days
Result: Enhances overall body growth promotion as well as the growth increase for tail, tibia, and femur.
分子量

569.46

Formula

C28H27Cl2FN6O2
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

FGFR2/3-IN-3 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:

FGFR2/3-IN-33069945-78-1Cytochrome P450FGFRCYPsFibroblast growth factor receptorInhibitorhERG cellsBa/F3 Cell LinesRT-112/84 cellFgfr3Y367C/+ mouse model of ACHEx vivo fetal mouse femur culture modelinhibitorinhibit

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：
FGFR2/3-IN-3
目录号：
HY-176547
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