PI3 Kinase p110 Alpha (PIK3CA) Drug Discovery Landscape & Assay Solutions
- By admin
- 30 Jul 2026
- Comments
Market Intelligence, Clinical Progress, and High-Purity Reagents for Precision Oncology Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for PIK3CA drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | PIK3CA WT & Mutant Recombinant Proteins (H1047R, E545K, C420R) High purity (>95%), Sequence Verified, Theoretical MW confirmed, Endotoxin <1EU/µg. |
View PIK3CA Products |
| Gene Delivery | PIK3CA Promise-ORF / Lentivirus Full-length ORF for stable cell line generation in engineered cancer models. |
View PIK3CA Products |
| Benchmark Ab | Anti-PIK3CA (Research Grade Detection Antibody) For Western Blot and Immunoprecipitation validation. |
View PIK3CA Products |
| Validator | PIK3CA siRNA Set For knockdown and specificity verification in cellular assays. |
View PIK3CA Products |
| Related Target A | PIK3CB (p110β) Isoform selectivity counter-screening for pan-PI3K inhibitor development. |
View PIK3CB Products |
| Related Target B | PTEN Companion pathway marker for resistance prediction and pathway activation studies. |
View PTEN Products |
| Related Target C | AKT1 Downstream effector for pathway engagement validation and feedback mechanism studies. |
View AKT1 Products |
| Related Target D | PIK3R1 (p85α) Regulatory subunit for holoenzyme complex formation assays. |
View PIK3R1 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Mutant vs WT Selectivity (H1047R, E545K) | Purified Mutant and WT Proteins available (>95% purity, Mass Spec verified) for selectivity assays |
| Isoform Selectivity (α vs β/γ/δ) | PIK3CB, PIK3CD, PIK3CG homolog proteins (>95% purity) for cross-reactivity screening |
| Resistance Mutation Surveillance | C420R, H1047L mutant proteins for next-generation inhibitor validation |
| Target Engagement & Pathway Readout | Anti-PIK3CA and Anti-pAKT1 recombinant antibodies for cellular target engagement |
| Assay Specificity Control | Validated siRNA included for genetic validation of target engagement |
Live PIK3CA R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for PIK3CA therapeutics is intensifying, with major players shifting focus from pan-PI3K inhibitors to highly selective, mutant-specific small molecules and degraders. As first-generation agents like alpelisib (Piqray) and inavolisib (Itovebi) establish clinical proof-of-concept in HR+ breast cancer, the next wave of R&D is targeting wild-type-sparing mechanisms to mitigate dose-limiting toxicities such as hyperglycemia, alongside rationally designed combination therapies with endocrine agents and CDK4/6 inhibitors.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule (α-Isoform Selective) | Novartis, Roche/Genentech | HR+ Breast, Endometrial, Colorectal | Kinase Selectivity Panel (Need PIK3CA mutant & WT proteins; PIK3CB, PIK3CD, PIK3CG homologs) |
| Small Molecule (Mutant-Selective) | Relay Therapeutics, Scorpion Therapeutics | PIK3CA-Mutant Solid Tumors | H1047R/E545K Mutant vs WT Selectivity Assay (Need sequence-verified mutant proteins) |
| PROTAC / Degrader | Arvinas, C4 Therapeutics, Cullgen | Resistant / Refractory Cancers | Cellular Degradation Assay (Need high-affinity binding antigens and lentivirus stable cell lines) |
| Combination Therapy | AstraZeneca, Daiichi Sankyo | HR+ Breast Cancer | Pathway Analysis (Need PTEN, AKT1, CDK4/6 combo reagents) |