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The aim was to design and discover a novel pan-KRAS inhibitor effective against various KRAS mutations.

Design and Discovery of BH-501242, a Novel Pan-KRAS On/Off Inhibitor Targeting KRAS Switch II Pocket

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The aim was to design and discover a novel pan-KRAS inhibitor effective against various KRAS mutations.
Utilized structure-based drug design to optimize a chemical scaffold targeting KRAS switch II pocket.
Conducted cellular anti-proliferation and anti-phosphorylation assays against KRAS mutant cell lines.
Performed pharmacokinetic profiling and evaluated bioavailability in mouse xenograft models.
BH-501242 exhibited sub-nM to low single-digit nM IC50 values across various KRAS mutations.
Demonstrated superior anti-proliferation activity in multiple cell lines with KRAS mutations.
Showed effective target engagement by blocking KRAS interaction with downstream c-RAF.

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Demonstrates a novel KRAS inhibitor enhancing anti-tumor activity in multiple cancer models, suggesting significant therapeutic potential.

Rui et al. (2026) studied this question.

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Demonstrates a novel KRAS inhibitor enhancing anti-tumor activity in multiple cancer models, suggesting significant therapeutic potential.