1. Neuronal Signaling Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. D5261

D5261 是一个有效的、类型III变构的 tropomyosin-related kinase A (TrkA) 抑制剂。

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D5261 Chemical Structure

D5261 Chemical Structure

CAS No. : 1574574-57-4

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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

D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor[1].

IC50 & Target

TrkA

 

体外研究
(In Vitro)

D5261 (0-10 µM, 72 h) displays favorable anti-proliferative activity in Ba/F3-MPRIP-TrkA cells (IC50 = 3.32 µM) and Ba/F3 CD74-TrkA cells (IC50 = 2.91 µM) [1].
D5261 exhibits cellular selectivity over TrkB/C to some extent (Ba/F3 IC50 > 10 µM, Ba/F3-QKI-TrkB IC50 = 6.17 µM and Ba/F3-EML4-TrkC IC50 > 10 µM)[1].
D5261 (0-50 µM) inhibits the TrkA autophosphorylation and downstream signaling in a concentration-dependent manner[1].
D5261 shows inhibitory activity against Ba/F3 cells harboring TrkA mutants (G667C, G667S, G667A, G595R and V573 M)[1].

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

Cell Viability Assay[1]

Cell Line: Ba/F3-MPRIP-TrkA, Ba/F3 CD74-TrkA cells
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Displayed favorable anti-proliferative activity with an IC50 of 3.32 and 2.91 µM against Ba/F3-MPRIP-TrkA and Ba/F3 CD74-TrkA cells, respectively.

Western Blot Analysis[1]

Cell Line: Ba/F3 CD74-TrkA cells
Concentration: 0.08, 0.4, 2, 10, and 50 µM
Incubation Time:
Result: Inhibited the TrkA autophosphorylation and phosphorylation of downstream PLCγ1, AKT and ERK in a concentration-dependent manner.
分子量

447.53

Formula

C25H29N5O3

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 *
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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:
D5261
目录号:
HY-144690
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