SML4057

PF-9363

≥98% (HPLC)

• Synonym(s): 2,6-Dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]benzenesulfonamide, CTx 648, CTx-648, CTx648, PF9363
• Empirical Formula (Hill Notation): C₂₀H₂₀N₄O₆S
• CAS Number: 2569009-58-9
• Molecular Weight: 444.46
• MDL number: MFCD34474252
• UNSPSC Code: 41106305
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Description

Biochem/physiol Actions

Orally active, highly potent and selective lysine acetyltransferase KAT6A inhibitor with anti-cancer efficacy in vivo.PF-9363 (CTx-648) is an orally active, highly potent and selective lysine acetyltransferase KAT6A inhibitor (KAT6A Ki = 0.27 nM; KAT6B/7/5/8 Ki = 2.4/70/420/670 nM). PF-9363 selectively inhibits H3K23 acetylation (ZR-75-1 H3K23Ac/H3K14Ac IC50 = 0.85/120 nM) and exhibits anti-proliferation potency against high KAT6A-expressing estrogen receptor signaling-positive (ER+) breast cancer cells in cultures (ZR-75-1 IC50 = 0.37 nM) and in mice in vivo (complete inhibition of ZR-75-1 xenograft tumor growth by 0.03 mg/kg/day p.o.) by downregulating cancr ER signaling, cell cycle and MYC transcriptional programs.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable