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 IC 50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers.
性状
Solid
IC50 & Target[1][2]
EGFR (WT) 7.92 nM (IC50) EGFR (C797S/T790M/L858R)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Ling WY, et, al. Prostaglandin E2 suppresses bacterial killing in alveolar macrophages by inhibiting NADPH oxidase. WO2019015655A1.
溶解度数据
In Vitro: 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)配制储备液