Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-

Biological Activity

PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer[1][2]. PF-9363 (0~1 μM; 1 day; ZR75-1, T47D and MCF7 cells) down-regulates the expression of H3K23Ac biomarker[1].PF-9363 leads to down regulation of a specific set of genes involved in ESR1 pathway, cell cycle and stem cell pathways. PF-9363 shows that the IC50 values for ZR75-1 and T47D are 0.3 nM and 0.9 nM[1]. PF-9363 shows strong anti-tumor activity in patient-derived xenograft models[1].

References

[1]. Shikhar S, et al. First-in-class KAT6A/KAT6B Inhibitor CTx-648 (PF-9363) Demonstrates Potent Anti-tumor Activity in ER+ Breast Cancer with KAT6A Dysregulation [2]. WO2020254946