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.

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.

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 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/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].

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].

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].

Dxd-d5, a deuterated derivative of Dxd, acts as a potent DNAtopoisomerase I inhibitor with an IC50 value of 0.31 μM. It serves as the effective payload for the antibody-drug conjugate (ADC) targeting HER2, known as DS-8201a.

Hersintuzumab is a humanized antibody produced in CHO cells, targeting ERBB2/HER2/CD340. It features a huIgG1 heavy chain and a huκ light chain, with an estimated molecular weight (MW) of 150 kDa. The isotype control for Hersintuzumab is available as [HumanIgG1kappa, Isotype Control].

LE01 is a component of the antibody-drug conjugate (ADC) known as a drug-linker conjugate for ADC. It comprises an ADC linker and the DNA topoisomerase I inhibitor DXd. LE01 is used in the synthesis of the HER2-targeting antibody-drug conjugate named HER2-LE01.

YH32367 (ABL105) is a bispecific antibody targeting HER2 and 4-1BB. It induces the secretion of IFN-γ, resulting in the death of tumor cells when co-cultured with hPBMC and HER2-expressing tumor cells. YH32367 demonstrates notable antitumor activity.

BAT1006 is a monoclonal antibody targeting the extracellular domain II of HER2, with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC). It is utilized for research in HER2-positive locally advanced/metastatic solid tumors. Compared to pertuzumab, BAT1006 exhibits roughly 5 times increased ADCC effect and demonstrates potent antitumor activity in HER2-positive Calu-3 xenograft mouse models.

COVA208 is a bispecific FynomAb targeting HER2, consisting of a fusion protein of an antibody and a FynSH3-derived binding protein. It induces the degradation of HER2, reducing the levels of HER2, HER3, and EGFR, effectively blocking downstream signaling pathways such as HER3-PI3K-AKT and MAPK, and inducing apoptosis in tumor cells. COVA208 shows promise for research in cancers like HER2-positive breast, gastric, and colorectal cancers.

NM-02 is a HER2-targeting antibody with an EC50 value of 1.2 nM. It binds to domains I and II of the HER2-ECD, inhibiting HER2-associated signaling pathways. NM-02 shows potential for research in HER2-positive breast cancer.