head and neck cancer

Borofalan(10B) (L-4-Boronophenylalanine) echibits antineoplastic effects. Borofalan can be used in studies on recurrent or locally advanced head and neck cancer.

Borofalan (also known as SPM 011) is an adjuvant compound used in boron neutron capture therapy (BNCT) for cancer treatment. BNCT leverages the high neutron capture cross-section of boron-containing compounds (10 B) and facilitates the 10 B(n,α) 7 Li neutron capture and nuclear fission reaction. With the use of borofalan (10B)-containing C-BENS, BNCT has demonstrated effective therapeutic potential in patients with R-SCC or R/LA-nSCC of the head and neck. Note: We offer the non-labeled version of Borofalan.

Wntpathway inhibitor 5 (Compound 28) is an effective wntpathway inhibitor with an IC50 value of less than 0.003 μM. This compound can suppress various types of cancers such as ovarian teratoma, breast cancer, osteosarcoma, and head and neck squamous cell carcinoma.

eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.

TrkA-IN-9 (VMD-928) is an orally active and selective inhibitor of tropomyosin receptor kinase A (TrkA). It disrupts downstream signaling pathways activated by nerve growth factor (NGF) binding to TrkA, thereby inhibiting cell proliferation and invasion, and promoting cancer cell death. TrkA-IN-9 shows potential for research in various cancers, including prostate cancer, thymic carcinoma, mesothelioma, head and neck squamous cell carcinoma, lung cancer, ovarian cancer, and hepatocellular carcinoma.

Cevimeline, a parasympathomimetic and muscarinic agonist, affects M1 and M3 receptors. Cevimeline has been shown to treat dry mouth and Sj gren's syndrome. It is also used to reduce Xerostomia symptoms and increase salivary flow in head and neck cancer survivors after radiotherapy.

EGFR-IN-165 is a potent EGFR inhibitor with IC50 values of 17.18 nM for EGFRL858R/T790M kinase and 64.74 nM for EGFRWT. Its IC50 values for NCI-H1975 and A431 cell lines are 2.17 μM and 6.2 μM, respectively. EGFR-IN-165 significantly inhibits cell migration, induces G1 phase cell cycle arrest, and causes apoptosis. It is suitable for research on cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

SVC112 is a translation elongation inhibitor that obstructs the periodic dissociation of EF2 from the ribosome, thereby inhibiting the elongation phase of translation. It demonstrates inhibitory activity in multiple cancer cell lines, including acute myeloid leukemia (AML), multiple myeloma, colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC). SVC112 preferentially impedes ribosomal processing of mRNA, reducing cancer stem cell (CSC)-related proteins such as Myc and Sox2. In hematological cancer cell lines, it induces apoptosis, whereas in colorectal cancer lines, the phosphorylation of c-Myc correlates with sensitivity to SVC112. The compound effectively inactivates HNSCC stem cells in vitro and prevents tumor regrowth in mouse HNSCC xenograft models. SVC112 is applicable for research on head and neck squamous cell carcinoma.

Cystemustine is a DNA inhibitor that induces DNA cross-linking, thereby preventing tumor cell proliferation. It exerts cytotoxic effects by disrupting the cell cycle, inducing cell redifferentiation, and altering phospholipid metabolism. Cystemustine shows high antitumor activity and a short plasma half-life in mice, influenced by the timing of administration. It is applicable in research on various malignancies, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer.

LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.

EGFR-IN-59 is a potent and selective EGFR inhibitor. It downregulates PI3K/AKT/mTOR signaling by blocking receptor autophosphorylation, exhibiting significant anti-proliferative activity in A431 and NSCLC cells.

Edatrexate (CGP 30694), also known as 10-Ethyl-10-deazaaminopterin, is an analog of Methotrexate that demonstrates antitumor activity against Methotrexate-resistant tumors. This antifolate antimetabolite is utilized in research related to non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and head and neck cancer [1] [2].

NR2F1 agonist 1, a specific nuclear receptor NR2F1 activator, initiates dormancy programs in cancer cells by upregulating NR2F1 and its target genes controlling dormancy. This compound promotes neural crest-like features and suppresses growth in head and neck squamous cell carcinoma (HNSCC) through NR2F1 activation. Moreover, NR2F1 agonist 1 demonstrates tumor growth inhibition in a mouse primary tumor model.

Zalutumumab is a high-affinity fully human monoclonal antibody that targets the extracellular domain of the epidermal growth factor receptor (EGFR) and is used to treat squamous cell carcinoma of the head and neck (SCCHN).

Petosemtamab (MCLA 158) is a highly potent monoclonal antibody against EGFR (Kd: 0.22 nM) and LGR5 (Kd: 0.86 nM). Petosemtamab promotes EGFR signaling disruption and receptor breakdown in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

Izalontamab (SI-B001) is a bispecific EGFR/HER3 monoclonal antibody that binds to both EGFR×EGFR homodimers and EGFR×HER3 heterodimers, thereby blocking downstream pathways. It is applicable for locally advanced or metastatic epithelial tumours, such as non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC).

Lirilumab (IPH2102) is an antibody against the lethal immunoglobulin-like receptor antibody KIR2D with antitumor activity that enhances the anti-HPV + cervical cancer activity of natural killer cells through VAV1-dependent NF-κB deinhibition. It can be used to study leukemia, head and neck squamous cell carcinoma (SCCHN).

Depatuxizumab is a humanised monoclonal antibody targeting EGFR with blood-brain barrier (BBB) permeability, capable of inhibiting the growth of xenograft tumours expressing mutant EGFR vIII and wild-type EGFR. It can be conjugated with the ADC molecule Depatuxizumab mafodotin for the study of glioblastoma (GBM) and head and neck squamous cell carcinoma (SCCHN).

Pimurutamab (HLX-07) is a glycoengineered humanized IgG1 monoclonal antibody that specifically targets the Epidermal Growth Factor Receptor (EGFR/HER1). By binding to the extracellular domain of EGFR, Pimurutamab blocks ligand (e.g., EGF, TGF-α) binding, inhibiting receptor dimerization and downstream signaling cascades (e.g., RAS/RAF/MEK/ERK). Its optimized glycosylation profile significantly enhances Antibody-Dependent Cell-mediated Cytotoxicity (ADCC) activity. Pimurutamab is developed for treating EGFR-overexpressing solid tumors, such as colorectal cancer and head and neck squamous cell carcinoma, with potentially improved efficacy over cetuximab.

REGN-1400 is a fully human monoclonal antibody inhibitor targeting ErbB3. By inhibiting ErbB3, REGN-1400 blocks associated signaling pathways to reduce tumor cell proliferation. It shows potential for research in solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN).

CQY684 (PCA062 antibody) is a human monoclonal antibody (mAb) that targets CDH3/P-cadherin. It stabilizes the X-dimer of P-cadherin, facilitating its endocytosis and directing it towards lysosomal degradation. CQY684 is applicable in studies of breast cancer, esophageal cancer, and head and neck cancers.

Sym004 is a 1:1 mixture of two recombinant human-mouse chimeric monoclonal antibodies (mAb), targeting non-overlapping EGFR epitopes (mAb992 and mAb1024). This compound facilitates the rapid internalization of EGFR and mediates subsequent degradation of internalized receptors through EGFR cross-linking. Sym004 can be utilized in research concerning metastatic colorectal cancer, head and neck cancer (H&N), and lung cancer.

Petosemtamab (FUT8-KO) is a variant of Petosemtamab with the fucosyltransferase 8 gene (FUT8) knocked out. Petosemtamab is a monoclonal antibody (mAb) targeting EGFR (with a Kd of 0.22 nM) and LGR5 (with a Kd of 0.86 nM). This antibody disrupts EGFR signaling and causes receptor degradation in LGR5+ cancer cells. It is applicable in research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

N-Acetylgalactosamine-6-Sulfatase (GALNS) is a potential universal biomarker for several malignant tumors, including lung cancer, breast cancer, and head and neck cancer. Insufficient activity of N-Acetylgalactosamine-6-Sulfatase can lead to mucopolysaccharidosis type IVA (MPS IVA), also known as Morquio A syndrome. This enzyme is utilized in research related to MPS IVA and cancer.