AZD3759 - 10mM in DMSO, high purity , CAS No.1626387-80-1

Item Number

A421980

• Synonyms: AZD3759 | 1626387-80-1 | AZD-3759 | zorifertinib | (R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate | 67SX9H68W2 | AZD 3759 | UNII-67SX9H68W2 | 4-[(3-CHLORO-2-FLUOROPHENYL)AMINO]-7-METHOXYQUINAZOLIN-6-YL (2R)-2,4-DIMETH
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

AZD3759 is a potent, oral active, CNS-penetrantEGFRinhibitor withIC50of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.

Targets

EGFR (L858R) (Cell-free assay); EGFR (exon 19Del) (Cell-free assay); EGFR (WT) (Cell-free assay) 0.2 nM; 0.2 nM; 0.3 nM

In vitro

In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells.

In vivo

AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy.

Cell Research(from reference)

Cell lines：PC-9 (exon 19Del), H3255 (L858R) and H838 (wt) cells 

Concentrations：~30 mM 

Incubation Time：72 h