STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research.
STX-478 (0-10,000 nM; 1 h) demonstrates selectivity for MCF10A cells harboring the H1047R kinase-domain mutation[1].
STX-478 (30, 100 mg/kg; p.o.; single daily for 28 days) dose-dependently reduces tumor volume in a CAL-33 xenograft mice model[1].
References:
[1]. JR David St Jean, et al. Urea derivatives which can be used to treat cancer. Patent WO2022265993A1.