EGFR-IN-7

• CAT Number: I018597
• CAS Number: 2267329-76-8
• Molecular Formula: C32H41BrN9O2P
• Molecular Weight: 694.60
• Purity: ≥95%
• Synonyms: 5-bromo-4-N-(5-dimethylphosphorylquinoxalin-6-yl)-2-N-[2-methoxy-5-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine
• InChI: InChI=1S/C32H41BrN9O2P/c1-21-18-26(28(44-3)19-27(21)42-12-8-22(9-13-42)41-16-14-40(2)15-17-41)38-32-36-20-23(33)31(39-32)37-25-7-6-24-29(35-11-10-34-24)30(25)45(4,5)43/h6-7,10-11,18-20,22H,8-9,12-17H2,1-5H3,(H2,36,37,38,39)
• InChIKey: ZYSKXRAGBGLELB-UHFFFAOYSA-N
• SMILES: CC1=CC(=C(C=C1N2CCC(CC2)N3CCN(CC3)C)OC)NC4=NC=C(C(=N4)NC5=C(C6=NC=CN=C6C=C5)P(=O)(C)C)Br

EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers[1].
EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively[1].
EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM[1].
EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM[1].
EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM[1].
EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o.; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model[1].
EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model[1].

Reference

[1]. Ling WY, et, al. Prostaglandin E2 suppresses bacterial killing in alveolar macrophages by inhibiting NADPH oxidase. WO2019015655A1.