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

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

For research use only. We do not sell to patients.

D5261 Chemical Structure

D5261 Chemical Structure

CAS No. : 1574574-57-4

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D5261 Related Antibodies

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Description

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

IC50 & Target

TrkA

 

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].

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

D5261 Related Antibodies

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.
Molecular Weight

447.53

Formula

C25H29N5O3
CAS No.
SMILES

CC1=C(C=C(C=C1)C(NC2=CN=C(C=C2)N3CCN(C3=O)C4CCCC4)=O)N5CCCC5=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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D5261 Related Classifications

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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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