p-egfr

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.

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.

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).

(Rac)-PROTAC PARP/EGFR ligand 1 is a compound that includes ligands for target proteins PARP and EGFR, along with a PROTAC linker that recruits E3 ligases such as VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC DP-C-4, a dual CRBN-based PROTAC designed for the concurrent degradation of EGFR and PARP.

EGFRvIII peptide, a synthetic peptide mirroring the EGFRvIII fusion junction—a tumor-specific, perpetually active EGFR variant missing amino acids 6-273 of the wild-type—binds to HLA-A*0201-positive T2 cells under MHC class I at 25 µg/ml. It enables antigen presentation in dendritic cells from human peripheral blood mononuclear cells (PBMCs), thus activating CD8+ cytotoxic T lymphocytes and prompting IFN-γ production. Administered at 15 µg/animal with the TLR5 agonist flagellin B, EGFRvIII peptide elevates CD8+ T cell numbers, lowers regulatory T cells (Tregs) in the brain, diminishes tumor volume, and extends survival in a GL261 glioblastoma mouse model.

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.

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.

Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor capable of crossing the blood-brain barrier. It suppresses the p-EGFR, p-AKT, and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) demonstrates antitumor activity in the H1975-luc BM xenograft model in mice and is applicable for researching non-small cell lung cancer.

EGFR/c-Met-IN-1 (compound TS-41) is a dual inhibitor targeting EGFR and c-Met, with IC50 values of 68.1 nM for EGFRL858R and 0.26 nM for c-Met. EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, and reduces phosphorylation of EGFR, c-Met, and downstream AKT. This compound effectively inhibits tumor growth both in vitro and in vivo.

EP26 is an orally active and potent inhibitor of EGFR and PD-L1, with IC50 values of 48.6 nM and 1.77 µM, respectively. It reduces the protein expression of p-EGFR and induces cell cycle arrest at the G0/G1 phase. EP26 shows potential for glioblastoma research.

EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor, with an IC50 value of 18.94 nM. It induces apoptosis and causes G1 phase arrest. Additionally, EGFR-IN-175 downregulates the expression of p-EGFR, p-AKT, and p-ERK. It is applicable in cancer research, including studies on lung cancer.

ZW-49 is a pan-EGFR inhibitor with oral bioavailability, showing IC50 values ranging from 0.03 to 1.5 nM. It effectively inhibits all EGFR mutant subtypes and demonstrates selectivity for wild-type EGFR and other target families. ZW-49 blocks the ATP binding site and occupies a conserved hydrophobic sub-pocket, preventing steric clashes with P-loop mutations (PACC). It suppresses cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis, and exhibits antiproliferative activity in xenograft mouse models. ZW-49 is applicable in cancer research, including studies on non-small cell lung cancer.

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

4-Hydroxycinnamamide is a natural cinnamic acid derivative that can be isolated from plants such as Berberis pruinosa. 4-Hydroxycinnamamide exhibits α-glucosidase inhibitory activity.

Cys-GE11 is a cysteine-modified short peptide. It can link with PEG-P(TMC-DTC) through the N-terminus of cysteine to form a targeting polymer. Cys-GE11 targets cells with high EGFR expression, such as SMMC-7721 cells. This compound significantly enhances drug accumulation at tumor sites and exhibits low toxicity.