KIT (CD117 / c-Kit) Drug Discovery Landscape & Assay Solutions

Market Intelligence, Clinical Progress, and High-Purity Reagents for Oncology, Mastocytosis, and Stem Cell Conditioning Development.

TarMart Solution Ecosystem & Related Targets

Comprehensive reagent toolkit for KIT drug discovery. Select your modality below:

Component / Network Product Description Product Link
Antigen (WT) KIT ECD-Fc Fusion Protein
Human/Mouse/Cyno orthologs. Sequence Verified. High Purity (>95%). Endotoxin <1EU/μg. HEK293 Expressed (Native Glycosylation).
View KIT Products
Antigen (Mutants) KIT Mutant Proteins (D816V, V560G, Δ550-557, V654A)
Recombinant activation loop, juxtamembrane, and kinase domain mutations for resistance screening.
View KIT Products
Gene Delivery KIT Lentivirus Particles / ORF Clone
Full-length wild-type ORF with reporter markers (GFP/Puro) for stable cell line construction (Ba/F3, CHO). High-titer premade particles.
View KIT Products
Benchmark Ab Anti-KIT Reference Antibodies (Clone YB5.B8; Sequence of Barzolvolimab / Briquilimab)
Recombinant chimeric positive controls for binding, internalization, and functional assays.
View KIT Products
Validator KIT siRNA Set (3 unique targets)
Validated knockdown sequences for specificity confirmation in cellular assays.
View KIT Products
Related Target PDGFRA
Type III RTK homolog; co-mutated in GIST. Crucial for selectivity profiling and combination therapy.
View PDGFRA Products
Related Target FLT3
Type III RTK homolog; AML pathway overlap; essential for counter-screening.
View FLT3 Products
Related Target SCF (KIT Ligand)
Natural ligand for competitive binding assays and receptor activation studies.
View SCF Products
Related Target CD47
Synergistic macrophage checkpoint target for non-genotoxic conditioning regimens.
View CD47 Products
Critical Assay Challenge The TarMart Advantage (Technical Spec)
Resistance Mutation Profiling (D816V, V560G, V654A, Exon 11/17) Comprehensive KIT Mutant Panel (mass-spec verified, endotoxin controlled) for selectivity and resistance screening.
Selectivity over PDGFRA/FLT3 (Type III RTK Family) Homolog Panel (KIT/PDGFRA/FLT3/CSF1R) with >95% purity; Sequence-verified ECDs for cross-reactivity ELISA/SPR.
Cross-species Cyno/Mouse Efficacy & Tox Evaluation Human/Mouse/Cyno KIT ortholog proteins with native species-specific glycosylation (HEK293 expressed).
ADC Internalization & ADCC/ADCP Assessment High-purity KIT ECD-Fc with native conformation; suitable for FACS internalization and effector function assays.
False Positive Elimination in Cellular Assays Validated KIT siRNA set for target-specificity verification.
Lack of Reliable Positive Controls Clinical Benchmark Antibodies (YB5.B8, Barzolvolimab biosimilar, Briquilimab biosimilar) included for direct affinity/functional comparison.

Live KIT (CD117) R&D Tracker

Market data changes daily. Access the latest global pipeline status directly:

Global Clinical Landscape & Future Outlook

The therapeutic landscape for KIT-driven malignancies is transitioning from first-generation multi-kinase inhibitors to highly selective mutant-specific inhibitors, antibody-drug conjugates (ADCs), and monoclonal antibodies for non-oncology indications. While imatinib revolutionized GIST treatment, acquired resistance mutations—particularly in the activation loop (D816V) and juxtamembrane domain—have necessitated next-generation small molecules such as avapritinib and ripretinib. Concurrently, first-generation TKI therapies are reaching maturity, driving a wave of R&D into non-oncology indications: non-genotoxic stem cell conditioning (replacing toxic chemotherapy prior to bone marrow transplants) and chronic immunological disorders like severe mastocytosis and chronic spontaneous urticaria. Key trends include:

  • Mutation-specific inhibition: Compounds capable of distinguishing between primary and secondary resistance mutations (e.g., D816V vs. V560G).
  • Non-genotoxic conditioning: Monoclonal antibodies like Briquilimab (Jasper Therapeutics) are pioneering targeted stem cell depletion for safer HSCT and gene therapy.
  • Immunology expansion: Barzolvolimab (Celldex Therapeutics) targets mast cell-driven diseases (chronic urticaria, prurigo nodularis).
  • ADC development: Leveraging KIT internalization for targeted payload delivery in GIST, AML, and melanoma.
  • Combination strategies: KIT/PDGFRA dual targeting in GIST; KIT/FLT3 axis in AML; Anti-KIT + Anti-CD47 for enhanced macrophage-mediated clearance.

Competitive Modality & Indication Snapshot

Modality Representative Players Key Indications Critical Assay Need (Why TarMart?)
Small Molecule (Type I/II TKI) Novartis, Deciphera, Blueprint Medicines GIST (1st-3rd line), Advanced Systemic Mastocytosis Mutant vs WT Selectivity (Need D816V, V560G, Exon 11/17 mutant proteins)
Allosteric Inhibitor Novartis, Relay Therapeutics Imatinib-resistant mutations Conformational state binding (Need full-length lentivirus cell assays)
Monoclonal Antibody (Conditioning) Jasper Therapeutics (Briquilimab) Stem Cell Transplant, SCID, AML ADCC/ADCP assays (Need HEK293-expressed ECD with native glycans)
Monoclonal Antibody (Immunology) Celldex Therapeutics (Barzolvolimab) Chronic Urticaria, Prurigo Nodularis Receptor blocking assays (Need pure SCF ligand and KIT ECD)
ADC (Antibody-Drug Conjugate) Daiichi Sankyo (DS-6157), Celldex, Early-stage Biotech GIST, AML, Melanoma Internalization assay (Need stable cell lines via TarMart Lentivirus)
Bispecific Preclinical (Academic/Institutional) Immunotherapy combinations Homodimer/Heterodimer validation (Need cross-reactive species orthologs)