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Osimertinib Impurity 28

Product Name
Osimertinib Impurity 28
CAS No.
1638281-44-3
Chemical Name
Osimertinib Impurity 28
Synonyms
D6-Osimertinib;2H6]-Osimertinib;Osimertinib Impurity 28;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
CBNumber
CB78232303
Molecular Formula
C28H33N7O2
Formula Weight
499.62
MOL File
1638281-44-3.mol
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Osimertinib Impurity 28 Property

form 
Solid
color 
White to light yellow
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Hazard and Precautionary Statements (GHS)

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Osimertinib Impurity 28 Chemical Properties,Usage,Production

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

Osimertinib Impurity 28 Preparation Products And Raw materials

Raw materials

Preparation Products

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