Covalent FLT3 Inhibitor FLC-8 Potency and Selectivity Data

A research dataset from figshare details the discovery of FLC-8, a covalent inhibitor targeting the Cys807 residue in the FLT3 kinase for acute myeloid leukemia. It reports IC50 values for FLT3-WT (10.2 nM), G697R (11.6 nM), and N676D (24.1 nM) mutants, along with in vivo tumor growth inhibition data. The dataset was authored by Zi-Xuan Wang and last updated in April 2026.

Use Cases

• Analyze IC50 values for FLT3-WT and mutant variants (G697R, N676D) to compare compound potency.
• Evaluate tumor growth inhibition (TGI) percentages (136-178%) from MV4-11 xenograft studies for in vivo efficacy.
• Assess kinome profiling data for FLC-8's narrow inhibition spectrum to understand selectivity.
• Study covalent engagement metrics (mass spectrometry, peptide mapping) confirming Cys807 targeting.

Strengths

• Reports specific, low-nanomolar IC50 values (e.g., 10.2 nM for FLT3-WT).
• Includes in vivo efficacy data with quantified tumor growth inhibition percentages.
• Provides evidence for covalent binding mechanism via multiple experimental confirmations.

Limitations

• Dataset size is only 3.4 KB, indicating extremely limited scope and likely summary data only.
• Unknown row count and column structure prevents assessment of data granularity.
• Data is specific to a single compound (FLC-8) and its derivatives, limiting generalizability.

Provenance

Source

figshare, authored by Zi-Xuan Wang.

Collection Method

Experimental research data from biochemical assays, kinome profiling, and xenograft studies.

Freshness

Last updated April 2026.