BBT-176 is an orally effective EGFR inhibitor. BBT-176 has inhibitory activity against multiple EGFR C797S mutant cell lines. BBT-176 is commonly used in cancer research.

BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC).

EGFR ligand-14-PEG3-Boc contains EGFR ligand and linker. EGFR ligand-14-PEG3-Boc can be used for the synthesis of SJF-1521.

CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers.

ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC).

Enozertinib (ORIC-114) hemihydrate is the inhibitor for EGFR that exhibits antineoplastic activity.

MRC-G-001 is a Genipin derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.

BIEGi-1 is a potent and selective binary inhibitor of EGFR that effectively blocks EGFR-catalyzed nucleotide exchange and disrupts the EGFR–Rheb interaction. It robustly inhibits both EGFR kinase activity and mTORC1 signaling in EGFR-mutant cancer cells. This compound exhibits significant anti-proliferative effects with an IC50 of 17 nM for PC9 and 20 nM for HCC827.

AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the active HER2-HER3 heterodimer, inhibits oncogenic downstream signalling in SK-BR-3 breast cancer cells.

Befotertinib mesylate (D-0316 mesylate) is third-generation tyrosine kinase inhibitor (TKI) of EGFR . It can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).

Asandeutertinib (Osimertinib-d3, AZD-9291-d3) is an orally administered, ATP-competitive, irreversible, deuterated third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR TKI) and a deuterium-stabilized derivative of osimertinib, with the potential to treat advanced EGFR-mutated NSCLC.

ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity.

TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.

Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor with IC50 and Ki values are 375 and 123 μM, respectively.

TX2-120-1 possesses the ability to bind to Her3, with an IC50 value of 56 nM for Her3. TX2-120-1 can be used for the synthesis of TX2-121-1, is a TNF-α inhibitor that inhibits endothelial. CC-1069 can be used to study angiogenesis-dependent tumors such as gliomas.

Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer.

JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab. JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163.

FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.

FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively.

Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively.

EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance.

DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 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). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models.

CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib.

BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells.

AZ14240475 is a potent, selective, and brain-penetrant inhibitor of EGFR Ex20Ins mutants, with the pIC50 of 7.6. AZ14240475 plays an important role in cancer research.

Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects.

Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis.

Andamertinib is the inhibitor for EGFR and exhibits antineoplastic activity.

4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates.

Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.