Preclinical Data for CPL423 TAM and FLT3 Kinase Inhibitor

Supplementary data from a preclinical study details the characterization of CPL423, a novel small-molecule inhibitor targeting TAM kinases and FLT3. The document reports sub-nanomolar IC50 values for MERTK (0.47 nM) and FLT3 (0.94 nM), and describes in vitro and in vivo efficacy in AML and melanoma models. The research was conducted by Agata Mikołajczyk and shared under a CC BY 4.0 license.

Use Cases

• Analyze reported IC50 values for MERTK and FLT3 to compare CPL423 potency against other kinase inhibitors.
• Review in vivo antitumor efficacy data from AML xenograft and A375 melanoma models for preclinical validation.
• Examine ADME/PK and cardiovascular safety liability profiles to assess the compound's drug-like properties.
• Study the ex vivo results on bone marrow derived dendritic cell (BMDC) phagocytic capacity for immune-modulation insights.

Strengths

• Reports specific, quantitative potency metrics, including sub-nanomolar IC50 values for key targets like MERTK (0.47 nM).
• Includes data from multiple experimental models: in vitro kinase assays, cell lines (MOLM-13, MV4-11), and in vivo xenografts.
• Provides a multifaceted characterization covering efficacy, selectivity, ADME/PK, and safety pharmacology.

Limitations

• The data is contained within a single 3.7 MB DOCX file, not a structured, machine-readable tabular format.
• Sample size details for in vivo studies (e.g., number of animals per group) are not explicitly stated in the provided description.
• The dataset's scope is limited to the specific compound CPL423, not a broader library of kinase inhibitors.

Provenance

Source

figshare, authored by Agata Mikołajczyk.

Collection Method

Experimental data generated from in vitro kinase assays, cell proliferation studies, in vivo xenograft models, and ex vivo phagocytosis assays.

Freshness

Last updated on 2026-03-25.