Market Intelligence, Clinical Progress, and High-Purity Reagents for Cell Cycle Inhibitor & Oncology Development.
TarMart Solution Ecosystem & Related Targets
"Comprehensive reagent toolkit for CDK2 drug discovery. Select your modality below:"
| Component / Network | Product Description | Product Link |
|---|---|---|
| Active Kinase Complex | CDK2/CCNE1 Complex Protein Active GST-tagged, High Purity (>95%), Sequence Verified, HEK293 Expressed, Endotoxin <1 EU/µg, Theoretical MW 60-65 kDa |
View CDK2 Products |
| Resistance Mutants | CDK2 Mutant Recombinant Proteins (F80C, T158A, F80A, and custom variants) Gatekeeper & T-Loop mutants for resistance screening, Sequence Verified |
View CDK2 Products |
| Gene Delivery | CDK2 Promise-ORF / Lentivirus Full-length ORF for stable cell line construction, High Titer |
View CDK2 Products |
| Validator | CDK2 siRNA Set (3 unique sequences) For knockdown verification & specificity control |
View CDK2 Products |
| Benchmark Ab | Anti-CDK2 Monoclonal Antibody Recombinant sequence, Suitable for Western/IHC |
View CDK2 Products |
| Related Target: CCNE1 | Cyclin E1 Protein (Regulatory Partner) Required for CDK2 activation, High Purity (>95%) |
View CCNE1 Products |
| Related Target: CDK1 | CDK1/CCNB1 Complex Paralog for selectivity counter-screening (avoid off-target toxicity) |
View CDK1 Products |
| Related Target: CDK4 | CDK4/Cyclin D1 Complex Family member selectivity testing |
View CDK4 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Selectivity over CDK1 (mitotic safety) | CDK1/CCNB1 Complex available with >95% purity for orthogonal testing; Sequence verified gatekeeper residue differences (F80 vs F86) |
| Drug Resistance Mutation Screening | CDK2 mutant panel (F80C, T158A, F80A) available; Sequence Verified; Theoretical MW matched |
| False Positive Controls | CDK2-specific siRNA Set included for cellular target validation |
| Active Complex Integrity | CDK2/CCNE1 pre-formed complex; Endotoxin Controlled (<1 EU/µg) for sensitive kinase assays |
Live CDK2 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for CDK2 therapeutics is intensifying, with major players shifting focus from pan-CDK inhibitors to highly selective CDK2 inhibitors and protein degraders. As first-generation ATP-competitive inhibitors enter Phase II (e.g., INCB123667 by Incyte, BLU-222 by Blueprint Medicines), the next wave of R&D is targeting allosteric inhibitors and PROTACs (e.g., CFT2718 by C4 Therapeutics) to overcome resistance mutations and improve selectivity over CDK1 to prevent mitotic catastrophe. The emergence of CDK4/6 inhibitor resistance (e.g., in HR+ breast cancer) has further positioned CDK2 as a synthetic lethal target, driving demand for sophisticated selectivity screening tools and combination strategies with PI3K/AKT or PARP inhibitors.
Critical clinical focus areas include CCNE1-amplified solid tumors (ovarian, endometrial, and triple-negative breast cancers) where CDK2 drives proliferation independent of CDK4/6. Future directions include PROTAC degraders (Arvinas, Nurix) and selective inhibitors from Relay Therapeutics (RLY-2608) targeting the same patient population.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Selective ATP-Competitive Inhibitors | Incyte, Blueprint Medicines (Novartis), Relay Therapeutics | CCNE1-amplified ovarian/endometrial cancer; HR+ breast cancer (post-CDK4/6i) | CDK1 Selectivity Assay (Need CDK2 vs CDK1 WT proteins) |
| PROTACs (Degraders) | C4 Therapeutics, Arvinas, Nurix Therapeutics | Solid tumors, Hematologic malignancies | Cell-Based Validation (Need CDK2 Lentivirus for stable lines) |
| Allosteric Inhibitors | Pfizer (discontinued but legacy), Biotech startups | Refractory solid tumors | Conformational Binding Assay (Need active vs inactive CDK2 complexes) |
| Covalent Inhibitors | Various Biotech | Resistance mutations | Cysteine mutant panel (Need F80C etc. for selectivity) |
Strategic Considerations for CDK2 Drug Development
Achieving best-in-class CDK2 inhibitors requires differentiation on multiple molecular axes:
- Selectivity over CDK1: CDK2 shares ~60% kinase domain homology with CDK1. Inhibition of CDK1 leads to mitotic catastrophe and unacceptable toxicity. Key residue differences (gatekeeper Phe80 vs Phe86) offer a selectivity handle. Assay strategy: Parallel screening against CDK1/CCNB1 using purified homolog panels.
- Overcoming resistance mutations: Gatekeeper mutation F80C (and F80A) and T-loop mutation T158A are known to reduce inhibitor binding. Fold-shift assays using mutant proteins are essential for resistance profiling.
- Complex integrity: Only CDK2 bound to Cyclin E1 or Cyclin A2 is catalytically active. Using pre-formed CDK2/CCNE1 complex ensures physiologically relevant screening.
- Mechanism of action: ATP-competitive (Type I) vs allosteric (Type III) vs PROTAC degraders each require distinct assay formats. TarMart provides active kinase complexes, mutant panels, lentivirus for stable lines, and siRNA for cellular validation.