Market Intelligence, Clinical Progress, and High-Purity Reagents for Oncology and Angiogenesis Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for EPHB4 drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | EPHB4 ECD-Fc / Mutant Protein High purity (>95%), Endotoxin <1EU/ug. Sequence Verified. HEK293 Expressed (Native Glycosylation). |
View EPHB4 Products |
| Gene Delivery | EPHB4 Promise-ORF / Lentivirus Full-length ORF for stable cell lines and internalization assays. |
View EPHB4 Products |
| Benchmark Ab | Anti-EPHB4 Recombinant Antibody Sequence Verified positive control for binding assays. |
View EPHB4 Products |
| Validator | EPHB4 siRNA Set For knockdown verification and specificity controls. |
View EPHB4 Products |
| Related Target: EFNB2 | Primary physiological ligand, critical for interaction and competition assays. | View EFNB2 Products |
| Related Target: EPHB2 | Highly homologous paralog, essential for selectivity counter-screening. | View EPHB2 Products |
| Related Target: EPHA2 | Family member often co-expressed in tumor microenvironment. | View EPHA2 Products |
| Related Target: VEGFR2 | Synergistic angiogenesis pathway for combination therapies. | View VEGFR2 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Eph Family Selectivity (EPHB4 vs EPHB2 vs EPHA2) | Ortholog panel proteins strictly verified by mass spec. Human/Mouse/Cyno ECD-Fc available with >95% purity. |
| Ligand Competition (EFNB2 blocking) | Recombinant EFNB2 and EPHB4 proteins available with >95% purity for precise SPR/BLI affinity screening. |
| ADC Internalization Efficiency | High-purity ECD-Fc preserves native conformational epitopes. Lentivirus stable cell lines for pH-sensitive internalization assays. |
| Cross-species Cyno/Mouse Testing | Human/Mouse/Cyno ortholog proteins structurally conserved and Sequence Verified. |
| False Positives / Off-target Binding | Validated siRNA included for specificity checks. Endotoxin controlled <1 EU/µg to eliminate LPS interference. Clinical Benchmark Antibodies included for direct comparison. |
Live EPHB4 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Molecular Characteristics of EPHB4
Based on UniProt P54760, EPHB4 (Ephrin type-B receptor 4) contains three functional domains: an Eph ligand-binding domain (Eph LBD) at the N-terminus, followed by two Fibronectin type-III domains (FN3-1 and FN3-2). These domains mediate ligand recognition, receptor dimerization, and downstream signaling. Key mutations include rs1584667224 (in CMAVM2, uncertain significance), rs34653459, and rs61735971 (also in CMAVM2, uncertain significance). Understanding these features is crucial for designing selective therapeutics and interpreting assay results.
Global Clinical Landscape & Future Outlook
The EPHB4 therapeutic landscape is transitioning from early-stage discovery to clinical validation, with antibody-drug conjugates (ADCs) leading the modality shift. Major players are shifting focus from traditional small molecule TKIs (e.g., NVP-BHG712) to Monoclonal Antibodies and next-generation ADCs and bispecifics. As a key regulator of tumor angiogenesis and lymphangiogenesis via forward and reverse signaling, EPHB4 represents a compelling target for solid tumors with high unmet medical need, including breast, ovarian, and prostate cancers. The first generation of angiogenesis inhibitors is reaching clinical maturity, and the next wave of R&D targets combination strategies with immunotherapy and novel payload technologies to overcome resistance. The competitive environment is intensifying around selectivity challenges given the high homology within the Eph receptor family (particularly EPHB2 and EPHA2). Bispecific approaches combining EPHB4 and VEGF pathways are gaining traction.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule TKI | Novartis, Array BioPharma | Solid Tumors | Selectivity Assay (Need Kinase Domain Proteins) |
| Monoclonal Antibody | VasGene Therapeutics | Breast, Ovarian Cancer | Ligand Blocking (Need High-purity ECD-Fc & EFNB2) |
| Bispecific / ADC | Various Biotech | Refractory Cancers | Internalization Assay (Need High-purity ECD-Fc) |
Strategic Implications and Assay Recommendations
For developing best-in-class therapies targeting EPHB4, researchers must address three critical differentiation points: (1) affinity and ligand blocking – use competitive SPR/BLI with recombinant EPHB4 ECD and EFNB2; (2) internalization efficiency for ADCs – employ cell-based assays with pH-sensitive dyes and stable cell lines; (3) subfamily selectivity – perform kinome profiling or cross-binding tests against homologous receptors. TarMart’s HEK293-expressed EPHB4 ECD-Fc protein preserves native glycosylation and conformational epitopes, making it ideal for sensitive SPR and internalization assays. The included siRNA and benchmark antibodies provide essential controls to reduce false positives and ensure data reliability.