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Chemical Structure : Utatrectinib
Catalog No.: PC-73452Not For Human Use, Lab Use Only.
Utatrectinib (AZD7451, AZ12607092) is a potent, selective, small molecule pan-Trk (NTRK) inhibitor with IC50 of 0.2-3.0 nM against TrkA, TrkB, and TrkC.
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Utatrectinib (AZD7451, AZ12607092) is a potent, selective, small molecule pan-Trk (NTRK) inhibitor with IC50 of 0.2-3.0 nM against TrkA, TrkB, and TrkC.
Binding of AZD7451 to TrkA, TrkB, and TrkC would be expected to inhibit responses associated with NGF, BDNF, and NT3, respectively.
AZD7451 completely blocked TrkC activation and associated tumorigenic behaviors at sub-micromolar concentrations in normal salivary gland tissue.
AZD7451 showed efficacy and low toxicity in pre-clinical studies on adenoid cystic carcinoma (ACC) tumors engrafted in mice.
AZD7451 potently inhibited in vitro growth and proliferation of the KM12 cell line harboring the NTRK1-fusion at 2 nM, AZD7451 inhibited proliferation of H460 cells at 5 nM, with TRKA phosphorylation inhibition.
| M.Wt | 382.403 | |
| Formula | C18H19FN8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ivanov SV, et al. Oncogene. 2013 Aug 8;32(32):3698-710.
2. Tatematsu T, et al. Mol Clin Oncol. 2014 Sep;2(5):725-730.
3. Li H, et al. J Cancer. 2019 Oct 15;10(24):6065-6073.
4. Tao Wang, et al. J Med Chem. 2008 Aug 14;51(15):4672-84.
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