1574574-57-4
1574574-57-4 structure
- Name: D5261
- Chemical Name: D5261
- CAS Number: 1574574-57-4
- Molecular Formula: C25H29N5O3
- Molecular Weight: 447.53
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Trk Receptor
- Create Date: 2022-05-21 13:01:41
- Modify Date: 2024-01-04 05:43:13
-
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor[1].
| Name | D5261 |
|---|
| Description | D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor[1]. |
|---|---|
| Related Catalog | |
| 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]. 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. |
| References |
| Molecular Formula | C25H29N5O3 |
|---|---|
| Molecular Weight | 447.53 |