Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-
- Product Name
- Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-
- CAS No.
- 2569009-58-9
- Chemical Name
- Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-
- Synonyms
- CTX-3648;PF-9363 (CTx-648);PF-9363, 10 mM in DMSO;2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1 -ylmethyl)-1,2-benzoxazol-3-yl]benzenesulfonamide;2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-benzenesulfonamide;N-(6-((1H-Pyrazol-1-yl)methyl)-4-methoxybenzo[d]isoxazol-3-yl)-2,6-dimethoxybenzenesulfonamide;Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-;CTx-648,cancer,patient-derived,anti-tumor,HAT,CTx648,Inhibitor,HATs,selective,xenograft,CTx 648,Histone Acetyltransferase,PF9363,inhibit,PF 9363,potent,PF-9363
- CBNumber
- CB49014266
- Molecular Formula
- C20H20N4O6S
- Formula Weight
- 444.46
- MOL File
- 2569009-58-9.mol
Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]- Property
- Boiling point:
- 692.0±65.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 2mg/mL, clear (Warmed)
- form
- Solid
- pka
- 6.34±0.30(Predicted)
- color
- White to off-white
Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]- Chemical Properties,Usage,Production
Uses
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].
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].
in vivo
PF-9363 shows strong anti-tumor activity in patient-derived xenograft models[1].
IC 50
MOZ/MORF
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
Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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