| Identification | Back Directory | [Name]
N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-3-(5-isopropoxy-1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridin-5-amine | [CAS]
1079274-94-4 | [Synonyms]
AZD-7451
Utatrectinib
N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-3-(5-isopropoxy-1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridin-5-amine
3H-Imidazo[4,5-b]pyridin-5-amine, N-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-3-[5-(1-methylethoxy)-1H-pyrazol-3-yl]- | [Molecular Formula]
C18H19FN8O | [MDL Number]
MFCD31715411 | [MOL File]
1079274-94-4.mol | [Molecular Weight]
382.39 |
| Chemical Properties | Back Directory | [Boiling point ]
645.9±65.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.78±0.10(Predicted) | [color ]
Blue to blue-green |
| Hazard Information | Back Directory | [Uses]
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors[1]. | [in vivo]
Utatrectinib (50 mg/kg, p.o., daily) suppresses adenoid cystic carcinoma (ACC) tumor growth in ACCX6 xenograft nu/nu mice model[2].
| Animal Model: | Xenograft nu/nu mice models of human ACC: ACCX6 and ACCX9[2] | | Dosage: | 50 mg/kg | | Administration: | Oral administration, daily. | | Result: | Tumor growth inhibition (TGI): 64% (in ACCX6 model) |
| [References]
[1] Kozaki R, et al. Combined use of Trk inhibitor containing heterocyclic urea derivative, and other kinase inhibitor for treating cancer. WO2019049891 A1.
[2] Ivanov SV, et al. TrkC signaling is activated in adenoid cystic carcinoma and requires NT-3 to stimulate invasive behavior. Oncogene. 2013 Aug 8;32(32):3698-710. DOI:10.1038/onc.2012.377
[3] Tatematsu T, et al. Investigation of neurotrophic tyrosine kinase receptor 1 fusions and neurotrophic tyrosine kinase receptor family expression in non-small-cell lung cancer and sensitivity to AZD7451 in vitro. Mol Clin Oncol. 2014 Sep;2(5):725-730. DOI:10.3892/mco.2014.318 |
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