CN-3: Potency Data for a Next-Generation RET Inhibitor Against Multiple Mutations

387.8 KB of data from figshare describes CN-3, a potent RET inhibitor. The dataset, authored by Zi-Xuan Wang and last updated in May 2026, reports IC50 values below 5 nM against multiple clinically relevant RET mutants, including G810R/S/C and V804M. It includes results from cellular proliferation assays (e.g., TT cells, IC50 = 2.48 ± 0.78 nM) and in vivo xenograft studies.

Use Cases

• Evaluating drug candidate potency based on reported IC50 values against RET mutants.
• Studying mechanisms of drug resistance based on activity against solvent-front and gatekeeper mutations.
• Assessing kinase selectivity for drug design based on the described off-target activity profile.
• Validating in vitro to in vivo correlation using the described xenograft efficacy data.

Strengths

• Includes specific potency metrics, such as IC50 < 5 nM for all tested RET mutants.
• Reports detailed experimental results, including IC50 values for TT cells (2.48 ± 0.78 nM) and LC-2/ad cells (17.05 ± 4.90 nM).
• Covers multiple clinically relevant resistance mutations (G810R/S/C, V804M, Y806H, M918T).

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• The dataset is small (387.8 KB), indicating limited scope.

Provenance

Source

figshare

Collection Method

Likely contains experimental biochemical and cellular assay data from a research study.

Freshness

Last updated 2026-05-02 13:34:25; freshness should be verified.