2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. TRK-IN-34

TRK-IN-34 是一种具有口服活性的 TRKA 和 TRKC 突变体激酶抑制剂，对 TRKAG595R，TRKAG667C 的 IC50 分别为 0.75 nM 和 0.96 nM。TRK-IN-34 可在功能层面抑制 TRKAG595R 和 TRKAG667C 的激酶活性。TRK-IN-34 可抑制转染 TRKA 的细胞增殖，在异种移植模型中发挥肿瘤生长抑制作用并实现部分肿瘤消退。TRK-IN-34 可用于研究由 TRKAG667C 突变驱动的 TRK 抑制剂耐药性癌症。

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

TRK-IN-34

TRK-IN-34 Chemical Structure

CAS No. : 2489327-91-3

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

TRK-IN-34 相关抗体

Top Publications Citing Use of Products

查看 Trk Receptor 亚型特异性产品:

查看所有亚型
TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRK-IN-34 is an orally active TRKand TRKC mutant kinase inhibitor, with IC50 values of 0.75 nM and 0.96 nM against TRKAG595R and TRKAG667C, respectively. TRK-IN-34 inhibits the kinase activities of TRKAG595R and TRKAG667C at the functional level. TRK-IN-34 inhibits the proliferation of TRKA-transfected cells, exerts tumor growth-inhibitory effects and achieves partial tumor regression in xenograft models. TRK-IN-34 can be used to study TRK inhibitor-resistant cancers driven by the TRKAG667C mutation[1].

IC50 & Target[1]

TRKAG595R

0.75 nM (IC50)

TRKAG667C

0.96 nM (IC50)

TRKAF589L

0.44 nM (IC50)

TrkA

2.8 nM (IC50)

TrkCG623R

0.73 nM (IC50)

TrkCG696A

1.3 nM (IC50)

体外研究
(In Vitro)

TRK-IN-34 (compound 5c) 在人肝微粒体中表现出良好的代谢稳定性，半衰期长达 153.1 min[1]。
TRK-IN-34 (作用 3 天) 可强效抑制表达野生型或突变型 TRKA 融合蛋白的 Ba/F3 细胞增殖，对 CD74-NTRK1-WT，CD74-NTRK1-G595R，CD74-NTRK1-G667C 的 IC50 值分别为 3 nM，6 nM 和 17 nM[1]。
TRK-IN-34 (1.23-300 nM; 6 h) 可剂量依赖性地抑制表达野生型或突变型 TRKA 融合蛋白的 Ba/F3 细胞中 TRKA 及其下游信号蛋白 PLCγ1 和 ERK 的磷酸化[1]。
TRK-IN-34 可在无细胞酶分析实验中强效抑制野生型及突变型 TRK 激酶，对 TRKAG595R、TRKAG667C、TRKCG623R 和 TRKAF589L 等关键耐药突变体的 IC50 值分别为 0.75 nM，0.96 nM，0.73 nM 和 0.44 nM[1]。

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

TRK-IN-34 相关抗体:

Western Blot Analysis[1]

Cell Line: Ba/F3-CD74-NTRK1-WT, Ba/F3-CD74-NTRK1-G595R, and Ba/F3-CD74-NTRK1-G667C cells
Concentration: 1.23, 3.7, 11.1, 33.3, 100 nM (Ba/F3-CD74-NTRK1-WT and Ba/F3-CD74-NTRK1-G595R cells); 3.7, 11, 33, 100, 300 nM (Ba/F3-CD74-NTRK1-G667C cells)
Incubation Time: 6 h
Result: Reduced phosphorylation of TRKA, PLCγ1, and ERK in a dose-dependent manner across all three Ba/F3 cell lines (wild-type, G595R mutant, G667C mutant).
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-inf CL Tmax F
Rat[1] 1 mg/kg i.v. 5.0 h 174.2 ng/mL 563.7 ng·h/mL 1.8 L/h/kg / /
Rat[1] 5 mg/kg i.g. 4.0 h 282.7 ng/mL 1485.1 ng·h/mL / 2.0 h 56.2 %
Dog[1] 1 mg/kg i.v. 6.0 h 628.9 ng/mL 1557.0 ng·h/mL 0.68 L/h/kg / /
Dog[1] 5 mg/kg i.g. 6.8 h 564.3 ng/mL 4214.2 ng·h/mL / 1.7 h 52.7 %
体内研究
(In Vivo)

TRK-IN-34 (compound 5c) (30-60 mg/kg；p.o.；每日 2 次；连续 2 周) 在 Ba/F3-LMNA-TRKAG667C 异种移植瘤小鼠中表现出强效的、剂量依赖性抗肿瘤活性，30 mg/kg 剂量下的 TGI 为 91%，60 mg/kg 剂量下的 TGI 为 115%，且 6 只动物中有 4 只出现部分肿瘤消退[1]。

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

Animal Model: Ba/F3-LMNA-TRKAG667C xenograft[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; twice daily; 2 weeks
Result: Achieved a tumor growth inhibition (TGI) of 91% at 30 mg/kg.
Achieved a TGI of 115% with partial tumor regression observed in 4 out of 6 animals at 60 mg/kg.
分子量

420.36

Formula

C19H16F4N6O
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

TRK-IN-34 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:

TRK-IN-342489327-91-3Trk ReceptorTropomyosin related kinase receptorBa/F3 cellstrk inhibitor-resistant cancerTRKC-G623Rhuman TRKA G667CTRKA-F589Lxenograft modelshuman TRKA G595Rhuman liver microsomesTRKA mutant kinaseTRKA-transfected cellsInhibitorinhibitorinhibit

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：
TRK-IN-34
目录号：
HY-181780
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