1. Neuronal Signaling Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. TRK-IN-29

TRK-IN-29 (Compound B31) 是第二代 TRK 抑制剂 (对 TRKAG595R、TRKAF589L、TRKAG667C、TRKA 和 TRKCIC50 分别为 9 nM、0.6 nM、18 nM、5 nM、6 nM)。TRK-IN-29 抑制 TRKA 的磷酸化。TRK-IN-29 对 NTRK 融合阳性细胞具有良好的抗增殖活性。TRK-IN-29 具有出色的血浆稳定性和适中的药代动力学特性。

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TRK-IN-29

TRK-IN-29 Chemical Structure

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查看 Trk Receptor 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

TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKAG595R, TRKAF589L, TRKAG667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
4.7 nM
Compound: B31
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay
[PMID: 39033612]
BaF3 IC50
9.9 nM
Compound: B31
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay
[PMID: 39033612]
KM12 IC50
0.3 nM
Compound: B31
Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay
[PMID: 39033612]
MCF7 IC50
1150 nM
Compound: B31
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay
[PMID: 39033612]
体外研究
(In Vitro)

TRK-IN-29 对 Km-12, Ba/F3-TRKAG595R 和 Ba/F3-TRKAG667C 细胞表现出较好的抗增殖效果, IC50 值分别为 0.3, 4.7, and 9.9 nM[1]

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

分子量

402.37

Formula

C19H17F3N6O

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.

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产品名称:
TRK-IN-29
目录号:
HY-161819
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