EGFR-IN-7

Research use only, not for human use.

EGFR-IN-7 is a selective and potent EGFR kinase inhibitor.TQB3804 displayed potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM respectively, and has similar enzymatic activity for EGFRWT (IC50 = 1.07) to Osimertinib.

EGFR-IN-7 is a selective and potent EGFR kinase inhibitor.TQB3804 displayed potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM respectively, and has similar enzymatic activity for EGFRWT (IC50 = 1.07) to Osimertinib. It also showed expected anti-proliferative activity in 4 cell lines, Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), PC9 (EGFRd746-750), and A431 (EGFRWT), with IC50 of 26.8, 163, 45, and 147 nM, respectively.

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.EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM.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.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. Cell Proliferation Assay Cell Line:A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) suspension cells Concentration:1 mM; 10 μM-0.508 nM Incubation Time:3 days Result:Inhibited proliferation in cells.

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.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. Animal Model:Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)Dosage:5, 15, 45 mg/kg Administration:Oral administration, daily, for 13 days Result:Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice.Animal Model:Subcutaneous xenograft PC-9 (Δ19del) model Dosage:0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg Administration:Oral administration, once a day, 3 weeks Result:Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.

TQB3804

Angiogenesis

EGFR

EGFR

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2267329-76-8

694.6

C32H41BrN9O2P

>98% (HPLC)

DMSO:5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCL and heat to 60°C)

COc1cc(N2CCC(CC2)N2CCN(C)CC2)c(C)cc1Nc1ncc(Br)c(Nc2ccc3nccnc3c2P(C)(C)=O)n1

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(-20℃)

With Ice Pack

≥ 2 years