D5261

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

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D5261 Chemical Structure

CAS No. : 1574574-57-4

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•Related Small Molecules:

•Related Proteins:

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TrkA TrkB TrkC Trk

Biological Activity
Purity & Documentation
References
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Description

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

IC₅₀ & Target

TrkA

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]

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.

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.

1574574-57-4

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

Handling Instructions (2659 KB)

References

[1]. Jing Guo, et al. Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies. Eur J Med Chem. 2022 Jan 15;228:114022. [Content Brief]

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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