her2-targeting

Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.

Trastuzumab deruxtecan (T-DXd) is an antibody-active molecule conjugate (ADC) with anticancer and antitumor activity, which is composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2) coupled to a topoisomerase I inhibitor (DXd). Trastuzumab deruxtecan has an improved effect on the treatment of HER2-positive breast cancer and gastric cancer.

Disitamab vedotin (RC-48) is a newly developed antibody-active molecule conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2), consisting of Disitamab coupled to monomethyl auristatin E (MMAE) via a cleavable linker. Disitamab vedotin showed anti-tumor and anti-proliferative activities in gastric cancer cells with different HER-2 expression levels and inhibited the expression of HER-2 protein in gastric cancer cells.

ABP-102 (CT P72) is a tetravalent IgG1-[L]-scFv bispecific t-cell adduct (BiTE) that acts as a CD3 modulator and selective HER2 modulator for the selective targeting of HER2 overexpressing tumors. ABP-102 showed cytotoxicity in HER2-overexpressing models of breast and gastric cancers, while significantly decreasing activity against HER2 low level cells, twice as effective as rununmotamab.

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.

HSP90-IN-35 is an inhibitor targeting Hsp90, exhibiting anticancer activity. It demonstrates an IC50 ranging from 0.05 to 0.5 μM against Her2. Additionally, HSP90-IN-35 can be utilized in the synthesis of PROTAC.

EGFR/HER2-IN-17 (Compound 7h) is a dual inhibitor targeting the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2). This compound suppresses cancer cell proliferation by interacting with the binding pockets of EGFR and HER2, activating Caspase-3 and Caspase-8, and reducing the expression of Bcl-2, thus inducing apoptosis (apoptosis). EGFR/HER2-IN-17 holds potential for cancer research.

ORM-5029 is the first antibody-drug conjugate (ADC) targeting the human epidermal growth factor receptor 2 (HER2), combining the highly potent GSPT1 degrader SMol006 with Pertuzumab. It is applicable in cancer research.

EGFR/HER2-IN-18 is a stable dual inhibitor targeting EGFR and HER2, with IC50 values of 0.09 μM and 0.08 μM, respectively. It exhibits broad-spectrum anticancer activity and can induce apoptosis and inhibit the cell cycle in MCF-7 cells. EGFR/HER2-IN-18 is applicable for breast cancer research.

EGFR/HER2-IN-19 (Compound L1) is a dual inhibitor targeting epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It holds potential for research into cancers driven by EGFR/HER2.

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

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].

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/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].

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

(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].

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

Anbenitamab (KN-026) is a novel Fc-fused bispecific antibody targeting the human epidermal growth factor receptor 2 (HER2). It simultaneously binds to two non-overlapping extracellular domain epitopes of HER2 (domain IV, targeted by trastuzumab, and domain II, targeted by pertuzumab). This biparatopic binding mode induces superior receptor clustering and rapid degradation, leading to potent inhibition of downstream signaling pathways such as MAPK and PI3K. Anbenitamab demonstrates significant anti-tumor activity in HER2-positive or low-expressing breast, gastric, and gastroesophageal junction cancers, and effectively mediates antibody-dependent cellular cytotoxicity (ADCC).

Zenocutuzumab (MCLA-128) is a humanized antibody targeting the extracellular domains of HER2 and HER3. It can be used for research on tumors driven by NRG1 gene rearrangement.

Timigutuzumab (GEXMab73) is a glyco-optimized monoclonal antibody targeting the human epidermal growth factor receptor 2 (ErbB2/HER2). Through glyco-engineering (typically afucosylation), the antibody's Fc region exhibits enhanced binding affinity for the FcγRIIIa receptors on immune effector cells, such as natural killer (NK) cells. This optimization significantly boosts Antibody-Dependent Cell-mediated Cytotoxicity (ADCC), enabling potent tumor cell lysis even in cases with low HER2 expression levels. Timigutuzumab is designed to overcome resistance to conventional anti-HER2 therapies and provide an improved therapeutic option for solid tumors.

Gancotamab (MM-302) is a HER2-targeting polyethylene glycolated liposome that encapsulates adriamycin to facilitate delivery to HER2-overexpressing tumor cells while limiting exposure to non-target tissues, including the heart.Gancotamab has antitumor activity and may be used to study advanced HER2-positive breast cancer.

Inetetamab is a humanized monoclonal antibody targeting HER2 receptor domain IV, exhibiting antitumor activity through inducing pyroptosis in lung adenocarcinoma. It is used in studies of HER2-positive metastatic breast cancer.

Coprelotamab (GB221) is a humanized IgG1 monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2/ERBB2), which effectively blocks receptor dimerization and downstream proliferative signaling by specifically binding to the HER2 extracellular domain IV. This antibody not only disrupts the malignant cell cycle but also possesses potent antibody-dependent cellular cytotoxicity (ADCC), enabling the precise elimination of HER2-overexpressing tumor lesions by recruiting immune effector cells.

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].