PF-9363, also known as CTx-648, is a first-in-class potent and high selective KAT6A/KAT6B inhibitor with efficacy against KAT6A-high ER+ breast cancer. CTx-648 (PF-9363), PF-9363 demonstrates anti-tumor activity in correlation with H3K23Ac inhibition in KAT6A over-expressing breast cancer. Transcriptional and epigenetic profiling studies show reduced RNA Pol II binding and downregulation of genes involved in estrogen signaling, cell cycle, Myc and stem cell pathways associated with CTx-648 anti-tumor activity in ER-positive (ER+) breast cancer. CTx-648 treatment leads to potent tumor growth inhibition in ER+ breast cancer in vivo models, including models refractory to endocrine therapy, highlighting the potential for targeting KAT6A in ER+ breast cancer.
MedKoo Cat#: 124375
Name: PF-9363
CAS#: 2569009-58-9
Chemical Formula: C20H20N4O6S
Exact Mass: 444.1104
Molecular Weight: 444.46
Elemental Analysis: C, 54.05; H, 4.54; N, 12.61; O, 21.60; S, 7.21
The following data is based on the product molecular weight 444.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
