Catalog No.: PC-24172Not For Human Use, Lab Use Only.
Pruvonertinib (YK-029A) is potent, wild-type sparing and mutant-selective inhibitor of EGFR T790 M and exon 20 insertion mutations with IC50 of 0.37 nM (EGFR L858R/T790 M), 29-fold selective over EGFR wt.
Pruvonertinib (YK-029A) is potent, wild-type sparing and mutant-selective inhibitor of EGFR T790 M and exon 20 insertion mutations with IC50 of 0.37 nM (EGFR L858R/T790 M), 29-fold selective over EGFR wt. YK-029A exhibits superior ntiproliferation effects in PC-9 (EGFRdel19), HCC827 (EGFRdel19), H1975 (EGFRLR/TM), and Ba/F3 (EGFRex20ins) cell lines YK-029A also shows potent antiproliferation effects in EGFRex20ins expressing Ba/F3 cells with relatively good wt-EGFR selectivity (4-78 fold) in contrast to osimertinib. YK-029A reduces pEGFR levels in the presence of EGF stimulation in H1975 cells, with reduction of pAKT levels led to the concomitant reduction in the downstream pERK levels. YK-029A is effective with oral administration in vivo. YK-029A (80 mg/kg, oral) exhibited significant antitumor activity in EGFRex20ins-driven patients-derived xenograft (PDX) models, preventing tumor progression or causing tumor regression.
