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

CN-3 is a potent RET inhibitor with IC50 values below 5 nM against all tested clinically relevant RET mutants, including solvent-front, gatekeeper, hinge, and catalytic loop variants. The dataset, shared by Zi-Xuan Wang on figshare in May 2026, includes results from cellular proliferation assays and kinase profiling. It shows CN-3 selectively suppressed RET-driven cell lines like TT and LC-2/ad and demonstrated dose-dependent antitumor efficacy in xenograft models.

Use Cases

• Compare inhibitor potency across RET mutations based on reported IC50 values.
• Analyze kinase selectivity profiles based on the described off-target activity against a limited group of receptor tyrosine kinases.
• Evaluate cellular model responses based on proliferation data from TT, LC-2/ad, and Ba/F3 cells.
• Assess in vivo antitumor efficacy and tolerability based on the xenograft study results mentioned.

Strengths

• Includes specific potency metrics, such as IC50 < 5 nM for all tested RET mutants.
• Reports detailed cellular assay results, including IC50 values of 2.48 ± 0.78 nM for TT cells and 17.05 ± 4.90 nM for LC-2/ad cells.
• 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 very small at 4.8 KB, indicating limited scope.

Provenance

Source

Zi-Xuan Wang via figshare

Collection Method

Likely contains experimental results from biochemical assays, cellular proliferation tests, kinase profiling, and xenograft studies.

Freshness

Last updated 2026-05-02 13:34:24; freshness should be verified.