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Background Information:
AZD9291 (Osimertinib) is an oral, irreversible, potent and selective third generation tyrosine kinase inhibitor (TKI) targeting EGFR activating (EGFRm+) and resistance (T790M) mutations in advanced lung adenocarcinoma, while sparing wild-type EGFR. Thus, AZD9291 potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; <25nM) and EGFRm+/T790M (e.g. H1975; <25nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo; >500nM). It is currently in clinical trials.) is an oral, irreversible, potent and selective third generation tyrosine kinase inhibitor (TKI) targeting EGFR activating (EGFRm+) and resistance (T790M) mutations in advanced lung adenocarcinoma, while sparing wild-type EGFR. Thus, AZD9291 potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; <25nM) and EGFRm+/T790M (e.g. H1975; <25nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo; >500nM). It is currently in clinical trials.
Reference:
1. D. Cross, et al., Mol Cancer Ther 2013;12(11 Suppl):Abstract No: A109.
2. D. Cross, et al., AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer, Cancer Discovery, September 2014, 4; 1046.
3. M. R. V. Finlay, et al., Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor, J. Med. Chem., 2014, 57 (20), pp 8249–8267.
APIM050106: AZD9291 (OSIMERTINIB)
CAS No.: 1421373-65-0.
Molecular Formula: C28H33N7O2.
Molecular Weight: 499.6.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO, Ethanol and Water with 2.0 eq. of HCl.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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