Covalent FLT3 Inhibitor FLC-8 Biochemical and In Vivo Activity Data

2026 research by Zi-Xuan Wang reports the discovery of FLC-8, a covalent inhibitor targeting the Cys807 residue in the FLT3 kinase. The dataset includes in vitro IC50 values against FLT3-WT (10.2 nM), G697R (11.6 nM), and N676D (24.1 nM) mutants, along with in vivo xenograft tumor growth inhibition results (136–178% TGI at 10–50 mg/kg).

Use Cases

• Analyze the relationship between compound FLC-8 structure and its IC50 values against FLT3-WT and mutant kinases.
• Model the correlation between in vitro IC50 potency (e.g., 10.2 nM) and in vivo tumor growth inhibition efficacy (136–178% TGI).
• Use kinome profiling data on FLC-8's narrow inhibition spectrum for off-target prediction in drug safety assessment.
• Study covalent engagement metrics, such as mass spectrometry and peptide mapping results for Cys807 binding, to validate the mechanism of action.

Strengths

• Includes specific, quantitative biochemical potency data (IC50 values in low nM range).
• Contains in vivo efficacy results from xenograft models with reported Tumor Growth Inhibition percentages.
• Data supports a novel mechanism of action via covalent binding to a specific residue (Cys807).

Limitations

• Dataset is very small (351.3 KB), likely containing only summary results from a single study.
• No raw experimental data or individual sample-level records are provided, limiting deep statistical analysis.
• Focus is on a single compound (FLC-8) and target, limiting generalizability.

Provenance

Source

Zi-Xuan Wang via figshare.

Collection Method

Experimental biochemical and pharmacological assays from a published drug discovery study.

Time Range

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Freshness

Last updated in April 2026.

Geography

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