EGFR-IN-11 是第四代 EGFR-酪氨酸激酶抑制剂 (EGFR-TKI)，对三重突变的 EGFR^{L858R/T790M/C797S} 的 IC₅₀ 为 18 nM。EGFR-IN-11 显著抑制 EGFR 磷酸化，诱导细胞凋亡，将细胞周期阻滞在 G0/G1处。

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC 50 of 18 nM for triple mutant EGFR. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.

Solid

EGFR 18 nM (IC50)

EGFR-IN-11 (Compound D9; 0.0001-10 μM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 μM, respectively.
EGFR-IN-11 (0.01-1.00 μM for HCC827 cells; 0.1-10.00 μM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line.
EGFR-IN-11 (1 μM; 24 h) potently induces the apoptosis of HCC827 cells.
EGFR-IN-11 (1 μM; 24 h) induces cell cycle arrests in HCC827 cell.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888.

In Vitro: DMSO : 125 mg/mL (217.88 mM; Need ultrasonic)配制储备液