| Identification | Back Directory | [Name]
Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]- | [CAS]
2569009-58-9 | [Synonyms]
CTX-3648
2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1 -ylmethyl)-1,2-benzoxazol-3-yl]benzenesulfonamide
Benzenesulfonamide, 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]- | [Molecular Formula]
C20H20N4O6S | [MDL Number]
MFCD34474252 | [MOL File]
2569009-58-9.mol | [Molecular Weight]
444.46 |
| Chemical Properties | Back Directory | [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 | [InChI]
1S/C20H20N4O6S/c1-27-14-6-4-7-15(28-2)19(14)31(25,26)23-20-18-16(29-3)10-13(11-17(18)30-22-20)12-24-9-5-8-21-24/h4-11H,12H2,1-3H3,(H,22,23) | [InChIKey]
VNSQFPFWUAZOTQ-UHFFFAOYSA-N | [SMILES]
O=S(NC1=NOC2=CC(CN3N=CC=C3)=CC(OC)=C21)(C4=C(OC)C=CC=C4OC)=O |
| Hazard Information | Back Directory | [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 |
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