Osimertinib Impurity 28
Osimertinib Impurity 28 Basic information
- Product Name:
- Osimertinib Impurity 28
- Synonyms:
-
- Osimertinib Impurity 28
- 2H6]-Osimertinib
- N-[2-({2-[di(2H?)methylamino]ethyl}(methyl)amino)-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl]prop-2-enamide
- D6-Osimertinib
- CAS:
- 1638281-44-3
- MF:
- C28H33N7O2
- MW:
- 499.62
- Mol File:
- 1638281-44-3.mol
Osimertinib Impurity 28 Chemical Properties
- form
- Solid
- color
- White to light yellow
Osimertinib Impurity 28 Usage And Synthesis
Uses
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
in vivo
Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].
| Animal Model: | PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1] |
| Dosage: | 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models) |
| Administration: | p.o.; daily for 14 day |
| Result: | Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models. |
References
[1] Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. DOI:10.1158/2159-8290.CD-14-0337
[2] [2]Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. DOI:10.1158/1535-7163.MCT-17-1033
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