PF-9363

Names

[ Name ]:
PF-9363

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

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

[Target]

KAT6A/KAT6B[1]

[In Vitro]

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]. Western Blot Analysis[1] Cell Line: ZR75-1, T47D and MCF7 cells Concentration: 0~1 μM Incubation Time: 1 day Result: Down-regulated the expression of H3K23Ac biomarker.

[In Vivo]

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

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₀N₄O₆S

[ Molecular Weight ]:
444.46

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xn

Related Compounds

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