EGFR-IN-167 

EGFR-IN-1671 is a selective EGFR inhibitor with an IC₅₀ of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC₅₀ = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors^[1].

EGFR-IN-167 (Compound 26) (1 μM) exhibits excellent in vitro potency (IC₅₀ = 35/< 1.8 nM)^[1].
EGFR-IN-167 (1-100000 nM, 72 h) possesses good cytotoxic activity against both A431 and HCC827 cells (GI₅₀ = 260 nM and 64 nM, respectively) and potently inhibits malignant cell proliferation (GI₅₀ = 458 nM and 112.7 nM against H3255 (L858R) and Ba/F3 (C797S) cells, respectively)^[1].
EGFR-IN-167 (0.01-10 μM, 4 h) results in a sustained inhibition of EGFR phosphorylation even after wash-out in in A431 and HCC827 cells^[1].
EGFR-IN-167 possesses moderate microsomal stability (T_1/2 = 29.6 min) in mouse liver microsomes^[1].
EGFR-IN-167 (10 μM) possesses favorable metabolic properties, with the inhibition ratios for the five main CYP isozymes (CYP1A2, 2C9, 2C19, 2D6 and 3A4) being <50%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

467.47

C₂₀H₂₂FN₃O₇S

3052761-67-5

O=S(OC1=CC=CC(NC2=C3C=C(OCCOC)C(OCCOC)=CC3=NC=N2)=C1)(F)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Tang G, et al. Cell-active, irreversible covalent inhibitors that selectively target the catalytic lysine of EGFR by using fluorosulfate-based SuFEx chemistry. Eur J Med Chem. 2023 Nov 5;259:115671.  [Content Brief]