Epertinib

Research use only, not for human use.

Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively.

Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively; does not inhibit KDR, IGF1R, SRC, KIT, PDGFRβ; phosphorylation of EGFR and HER2 kinases in NCI-N87 cells with IC50 of 4.5 and 1.6 nM, shows growth inhibition of NCI-N87 cell with IC50 of 8.3 nM; shows potent antitumor activity over lapatinib in a variety of xenograft models, exhibits excellent activity and could be effective against bone and brain metastasis.Breast Cancer Phase 2 Clinical

S-222611;S222611

Angiogenesis

EGFR

EGFR

Cancer

Breast Cancer

908305-13-5

560.03

C30H27ClFN5O3

>98% (HPLC)

——

CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5

(R,Z)-1-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)but-2-yn-1-one O-morpholin-3-ylmethyl oxime

(-20℃)

With Ice Pack

≥ 2 years