EGFR-IN-82 

EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC₅₀ values of 0.09 and 0.06 nM for EGFR^{L858R/T790M/C797S} and EGFR^{Del19/T790M/C797S}, respectively. EGFR-IN-82 has no significant effect on EGFR^WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research ^[1].

0.09 , 0.06 nM (EGFR^{L858R/T790M/C797S}, EGFR^{Del19/T790M/C797S})

EGFR-IN-82 (compound 8a) (72 h) significantly inhibits the growth of Ba/F3-EGFR^{Del19/T790M/C797S} cells with the IC₅₀ value of 12.7 nM, but has no significant effect on the growth of A431 cells ^[1].

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

EGFR-IN-82 (Cmpound 8a) has better pharmacokinetic performance than Brigatinib (HY-12857) in vivo^[1].
EGFR-IN-82 (15 - 30 mg/kg；Oral gavage (p.o.)；14 - 21 days) exhibits moderate inhibition on PC9-EGFR ^{Del19/T790M/C797S} xenograft mice model, while presents a very strong tumor growth inhibition effect on tumor with high expression of EGFR^{Del19/T790M/C797S[1]}.

Pharmacokinetic Analysis in Male Balb/C mice Model^[1]

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

694.60

C₃₂H₄₁BrN₉O₂P

2568086-81-5

COC1=C(NC2=NC=C(Br)C(NC3=C(P(C)(C)=O)C(N=CC=N4)=C4C=C3)=N2)C=C(C)C(N5CCC(N6CC(N(C)C)C6)CC5)=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. 1. Yanliang Guo, et al. Design, synthesis and biological evaluation of phosphoroxy quinazoline derivatives as potential EGFRT790M/C797S inhibitors. Bioorganic & Medicinal Chemistry. Volume 90, 15 July 2023, 117338.