her2-targeting

pan-HER-IN-2 (Compound C6) is an orally active, reversible, broad-spectrum HER inhibitor that targets EGFR (IC50: 0.72 nM), HER4 (IC50: 2.0 nM), EGFRT790M (IC50: 8.2 nM), and L858R (IC50: 75.1 nM). pan-HER-IN-2 induces apoptosis and possesses anti-tumor effects.

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

Dxd (OQM5SD32BQ) is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC.

ErbB-2-binding peptide (HER2-binding peptide), a tumor-targeting peptide, shows significant potential for cancer research applications [1].

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

(R)-Afatinib ((R)-BIBW 2992), an isomer of Afatinib, is a potent, orally administered, irreversible inhibitor targeting the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFR wt, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R T790M, and 14 nM for HER2, holding potential for research into esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer [1].

EGFR HER2-IN-12 (compound 14b) serves as a dual inhibitor targeting EGFR and HER2, demonstrating 81% and 51% inhibition respectively at a concentration of 10 μM. This compound exhibits minimal toxicity towards A431 and MDA-MB-361 cancer cells [1].

EGFR HER2-IN-11 (compound 20), an orally active dual inhibitor targeting human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), demonstrates IC50 values of 7.7 nM and 22 nM, respectively. This compound shows strong antitumor efficacy, specifically inhibiting the proliferation of BT-474 cancer cells with a GI50 of 601 nM [1].

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.

Zenocutuzumab (MCLA-128) is a humanized bispecific IgG1 antibody with Fab arms targeting the extracellular domains of HER2 and HER3[1].

Anbenitamab (KN-026) is a bispecific antibody targeting extracellular domains II and IV of human HER2, blocking both ligand-dependent and independent signaling pathways. Its IgG1 Fc fragment activates FcRγIIIa, triggering strong antibody-dependent cell-mediated cytotoxicity (ADCC) and suppressing tumor cell growth. Anbenitamab shows promise for research in HER2-positive metastatic breast cancer (MBC) [1][2].

EGFR HER2-IN-7 is a highly selective and potent anticancer compound designed to target MCF-7 breast cancer cells by functioning as a dual inhibitor of EGFR HER2 kinases and DHFR (dihydrofolate reductase), with IC50 values of 0.18 μM for EGFR, 0.146 μM for HER2, and 0.907 μM for DHFR [1].

EGFR HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor targeting EGFR (IC50: 5.02 μM) and HER2 (IC50: 0.83 μM).

EGFR HER2 DHFR-IN-3 (compound 4c) is an efficacious dual inhibitor of EGFR HER2 with IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively, and also inhibits DHFR with an IC50 of 0.193 μM. It induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is an ADC targeting HER2, cleaved by histone B within tumor cells for selective targeting, exhibiting antitumor activity and applicable in cancer research, particularly for uterine and ovarian sarcomas [1].

EGFR HER2 DHFR-IN-1 is a highly selective and potent anticancer compound targeting MCF-7 breast cancer cells, acting as a multi-inhibitor for EGFR HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. It induces cell cycle arrest at the G1 S phase and apoptosis in cells [1].

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a conjugate that acts as an immune agonist targeting both HER2-TLR7 and HER2-TLR8 pathways [1].