D5261
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
For research use only. We do not sell to patients.
- CAS No.: 1574574-57-4
- Formula: C25H29N5O3
- Molecular Weight:447.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TrkA |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>10 μM
Compound: D5261
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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
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[PMID: 34871843] |
| BaF3 | IC50 |
>10 μM
Compound: D5261
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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
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[PMID: 34871843] |
| BaF3 | IC50 |
2.91 μM
Compound: D5261
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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
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[PMID: 34871843] |
| BaF3 | IC50 |
3.32 μM
Compound: D5261
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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
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[PMID: 34871843] |
| BaF3 | IC50 |
6.17 μM
Compound: D5261
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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
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[PMID: 34871843] |
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.
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Cell Line:Ba/F3-MPRIP-TrkA, Ba/F3 CD74-TrkA cells
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Concentration:0-10 µM
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Incubation Time:72 h
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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.
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Cell Line:Ba/F3 CD74-TrkA cells
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Concentration:0.08, 0.4, 2, 10, and 50 µM
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Incubation Time:
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Result:Inhibited the TrkA autophosphorylation and phosphorylation of downstream PLCγ1, AKT and ERK in a concentration-dependent manner.
Chemical Information
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CAS No. 1574574-57-4
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Molecular Weight 447.53
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Formula C25H29N5O3
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SMILES
CC1=C(C=C(C=C1)C(NC2=CN=C(C=C2)N3CCN(C3=O)C4CCCC4)=O)N5CCCC5=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
D5261 Related Classifications
HY-144690 Related Classifications
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