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Background Information:
AZ5104 is an active circulating metabolite of AZD9291. It shares the similar overall activity profile with AZD9219, but is more potent against mutant EGFR forms, while hitting the wild-type EGFR form at a lower concentration thus demonstrating a smaller selectivity margin compared with the parent. Like AZD9291, AZ5104 displays potent antitumor activities both in vitro and in vivo, and is clinically competent with the parent.
Reference:
1. 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.
APIM050087: AZ5104
CAS No.: 1421373-98-9.
Molecular Formula: C27H31N7O2?0.3HCl.
Molecular Weight: 500.2.
Purity: >99% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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