EGFR

Tyrphostin AG 879 (AG 879) effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.

Desmethyl Erlotinib hydrochloride (OSI 420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor.

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells.

lavendustin A (RG-14355) is a potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.

EGF Rligand-11, a target protein ligand for EGFR, is utilized in the synthesis of PROTAC MS154.

RG14620 (Tyrphostin RG14620) is an epidermal growth factor receptor (EGFR) inhibitor.

BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs).Cost-effective and quality-assured.

1,5-Dihydroxyxanthone inhibits EGFR-tyrosine kinase (IC50: 90.34 nM) and may block AChE/BChE.

DA-0157 is an orally active inhibitor targeting EGFR and ALK, designed to overcome resistance mutations in non-small cell lung cancer (NSCLC). It effectively inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50= 6.9 nM), Ba/F3-EGFR WT (IC50= 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50= 5.5 nM), and Ba/F3-EML4-ALK (IC50= 7.4 nM). Additionally, DA-0157 inhibits CYP2D6 with an IC50 of 5.26 μM and demonstrates antitumor activity in mouse models.

EGFR-IN-127 is an ATP-competitive inhibitor targeting EGFR, with IC50 values of 136.3 nM for EGFRdel19 and 161.2 nM for EGFRdel19/T790M/C797S. This compound holds potential for the study of non-small cell lung cancer (NSCLC).

EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.

IBI-334 is a bispecific antibody targeting both B7-H3 and EGFR. It features an EGFR arm responsible for signal blocking, connected to a modified B7-H3 arm that ensures optimal affinity and binding. The antibody is afucosylated to enhance its antibody-dependent cellular cytotoxicity (ADCC) effects. IBI-334 is widely applicable in EGFR-driven solid tumors.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase.

CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and

Dalmitamig is a humanized IgG4κ antibody targeting EGFR/CD28, with HumanIgG4(S228P) kappa as its corresponding isotype control.

PD-149163 hydrochloride is a neurokinin B agonist with antipsychotic activity, used for research on neurological diseases.

Rilematovir (JNJ-678) inhibits fusion protein, has antiviral properties, low toxicity, and targets RSV treatment.

Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating

Allitinib tosylate (AST-1306) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively.

Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody with potential anti-tumor activity for the study of advanced malignant solid tumors.

Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR

Nimotuzumab is a humanized therapeutic monoclonal antibody against epidermal growth factor receptor EGFR).

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

H-9 dihydrochloride: Strong PKA inhibitor, curbs 5-HT response and EGF signaling, affects pharyngeal function.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator.Cost-effective and quality-assured.

Genistein (NPI 031L) is a natural soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor effects. Cost effective and quality assured.

YK-029A, an orally active EGFR mutant inhibitor, targets both EGFR T790M and EGFRex20ins mutations.

Antiproliferative Agent-34 (Compound A14), a multitarget kinase inhibitor, demonstrates IC50 values of 177 nM for EGFR L858R/T790M and 1567 nM for EGFR WT.

PD153035 (NSC-669364) hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR,

Rostafuroxin (PST 2238) has been used in trials studying the treatment of Essential Hypertension.

EGFR/HER2/DHFR-IN-2 (Compound 4b) serves as an inhibitor for EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively.

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.

Icotinib Hydrochloride, an oral EGFR inhibitor (BPI-2009H), may halt cancer growth by blocking EGFR signaling.

Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor.Cost-effective and quality-assured.

ALK/EGFR-IN-1 (Compound 8l) is a dual inhibitor targeting both ALK and EGFR, effectively blocking their phosphorylation.

EGFR-IN-11 selectively blocks EGFR-tyrosine kinase and promotes apoptosis; targets EGFRL858R/T790M/C797S, IC50=18 nM; halts cell cycle at G0/G1.

Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).

CP-380736 (PF-00520893) inhibits EGFR, a kinase key in cancer-signaling pathways like MAPK, JNK, and Akt.

Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant

Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).

Tyrphostin B44, (+) enantiomer is an inhibitor of epidermal growth factor receptor (EGFR) kinase with IC50 of 0.86 μM and has less active than the (-)

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.

Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and

(E)-AG 99 ((E)-Tyrphostin AG 99) is an inhibitor of EGFR kinase (IC50: 10 μM in the human epidermoid carcinoma cell line A431).

SST0116CL1 is an HSP90 inhibitor (IC50: 0.21 μM) that targets the ATP-binding pocket of Hsp90, disrupting its chaperone function and leading to the degradation of client proteins (EGFR, CDK4, and AKT). It induces the degradation of Her2 in BT-474 cells (IC50: 0.2 μM) and exhibits antiproliferative activity, inhibiting tumor growth.