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

Experimental data for CN-3, a potent RET inhibitor active against clinically relevant resistance mutations. The dataset includes IC50 values for RET mutants and cellular models, such as TT cells (IC50 = 2.48 ± 0.78 nM) and LC-2/ad cells (IC50 = 17.05 ± 4.90 nM). It was authored by Zi-Xuan Wang and last updated on 2026-05-02.

Use Cases

• Evaluating drug potency against specific RET mutations based on reported IC50 values.
• Analyzing kinase selectivity profiles based on the described off-target activity.
• Studying downstream signaling effects based on the described blockade of RET autophosphorylation and SHC/AKT/ERK pathways.
• Assessing in vivo antitumor efficacy based on the described xenograft model results.

Strengths

• Reports specific potency metrics, including IC50 values less than 5 nM for all tested RET mutants.
• Includes data from multiple experimental models, such as TT, LC-2/ad, and Ba/F3 cells.
• Describes mechanistic insights into signaling pathway blockade and cellular effects like G0–G1 arrest.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Data may reflect experimental bias inherent to the specific research methodology.

Provenance

Source

figshare

Collection Method

Likely contains experimental results from biochemical and cellular assays.

Freshness

Last updated 2026-05-02 13:34:31; freshness should be verified.