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QLS1303 is a potent, selective, and orally bioavailable small molecule inhibitor of KIF18A (Kinesin Family Member 18A), developed by Qilu Pharmaceutical. It is specifically designed to target cancers characterized by chromosomal instability (CIN) and high levels of aneuploidy. KIF18A is a plus-end kinesin required for silencing mitotic checkpoints and aligning extra chromosomes in CIN-high cells; its inhibition leads to catastrophic chromosome mis-segregation and apoptosis in these cells while sparing normal diploid cells. In preclinical studies, QLS1303 demonstrated robust anti-tumor activity, including tumor regression in TP53-mutant/aneuploidy-high xenograft models, and showed significantly higher potency than the clinical-stage inhibitor AMG 650.
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