Information AZ5104, the demethylated metabolite of AZD-9291, is a potentEGFRinhibitor withIC50of Targets EGFR (L858R/T790M) ; EGFR (L861Q) ; EGFR (L858R) ; ErbB4 ; EGFR (wildtype) 15117, In vitro AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively. In vivo In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. Cell Research(from reference) Cell lines：H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT) cells Incubation Time：96 h
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AZ5104
Dangerous GoodsCAS number：1421373-98-9 molecular formula：C27H31N7O2
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| Chinese alias | - | ||
| English alias | 2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-5-((4-(1H-indol-3-yl)-2-pyrimidinyl)amino)-4-methoxyphenyl)- | AKOS025404698 | CCG-269587 | 2DWZ6SE1E1 | N-(2-[2-Dimethylaminoethyl-methylamino]-5-{[4-(1H-indol-3-yl)pyrimidin-2-yl]amino}-4-methoxy | ||
| CAS number | 1421373-98-9 | molecular formula | C27H31N7O2 |
| molecular weight | 485.58 g/mol | Exact mass | - |
| PSA | 98.400 Ų | logp | 4.465 |
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害 H317: 可能引起皮肤过敏反应
Statement of Preventive Measures：
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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