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编 号：F745880
分子式：C25H29N5O3
分子量：447.53
分子式：C25H29N5O3
分子量：447.53
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CAS No: 1574574-57-4
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生物活性：
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
体外研究：
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) .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).D5261 (0-50 μM) inhibits the TrkA autophosphorylation and downstream signaling in a concentration-dependent manner.D5261 shows inhibitory activity against Ba/F3 cells harboring TrkA mutants (G667C, G667S, G667A, G595R and V573 M).
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
体外研究：
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) .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).D5261 (0-50 μM) inhibits the TrkA autophosphorylation and downstream signaling in a concentration-dependent manner.D5261 shows inhibitory activity against Ba/F3 cells harboring TrkA mutants (G667C, G667S, G667A, G595R and V573 M).
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