p-egfr

EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.

WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.

JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).

WHI-P154 (Jak3 inhibitor ii) is a potent JAK3 inhibitor.

EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0 G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.

WHI-P180 (Janex 3) is a potent inhibitor of EGFR and Cdk2, with IC50 values of 4.0 µM and 1.0 µM, respectively.

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A PP2A p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.

EGFR C797S-IN-1 is a potent inhibitor targeting the EGFR-C797S mutation, with an IC50 value of 0.128 µM, exhibiting significant anti-proliferative and anti-tumor effects by inhibiting p-EGFR expression in a dose-dependent manner.

Dosimertinib-d3 is a potent, orally active inhibitor of EGFR, known to reduce the expression of p-EGFR and p-ERK proteins, thereby exhibiting antiproliferative and anti-tumor effects. It holds promise for research into non-small-cell lung cancer (NSCLC).

EGFRT790M L858R-IN-2 is a potent, selective inhibitor of EGFRT790M L858R, exhibiting IC50 values of 3.5 nM for EGFRT790M L858R and 1290 nM for EGFR WT. This compound effectively decreases the expression of p-EGFR, P-AKT, P-ERK1 2, and induces apoptosis as well as cell cycle arrest in the G1 phase, demonstrating anti-cancer activity [1].

YS-67 is an orally available, selective and potent EGFR inhibitor with antitumor activity, inhibits p-EGFR and p-AKT, and inhibits the proliferation of A549, PC-9, and A431 cells.YS-67 blocks cell cycle progression and induces apoptosis in the G0 G1 phase, and can be used in the study of non-small-cell lung cancer.

Sulforaphene is a natural product isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1 2, NF‐κB and other signa