2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. 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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D5261 相关抗体

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查看 Trk Receptor 亚型特异性产品:

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TrkA TrkB TrkC Trk

  • 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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
> 10 μM
Compound: D5261
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34871843]
BaF3 IC50
> 10 μM
Compound: D5261
Antiproliferative activity against mouse BaF3 cells expressing EML4 fused TRKC assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing EML4 fused TRKC assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34871843]
BaF3 IC50
2.91 μM
Compound: D5261
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34871843]
BaF3 IC50
3.32 μM
Compound: D5261
Antiproliferative activity against mouse BaF3 cells expressing MPRIP fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing MPRIP fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34871843]
BaF3 IC50
6.17 μM
Compound: D5261
Antiproliferative activity against mouse BaF3 cells expressing QKI fused TRKB assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing QKI fused TRKB assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34871843]
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.

D5261 相关抗体:

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

D5261 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:

D52611574574-57-4D 5261D-5261Trk ReceptorTropomyosin related kinase receptorBa/F3PLCγ1Allosteric inhibitorAKTERKInhibitorinhibitorinhibit

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目录号：
HY-144690
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