SML4016

PF-9363

≥98% (HPLC)

• Synonim(y): 2,6-Dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]benzenesulfonamide, CTx 648, CTx-648, CTx648, PF 9363, PF9363
• Wzór empiryczny (zapis Hilla): C₂₀H₂₀N₄O₆S
• Numer CAS: 2569009-58-9
• Masa cząsteczkowa: 444.46
• UNSPSC Code: 12352200
• MDL number: MFCD34474252
• NACRES: NA.21
• Assay: ≥98% (HPLC)
• Form: powder

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Warmed)
• storage temp.: 2-8°C
• SMILES string: O=S(NC1=NOC2=CC(CN3N=CC=C3)=CC(OC)=C21)(C4=C(OC)C=CC=C4OC)=O
• 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)
• InChI key: VNSQFPFWUAZOTQ-UHFFFAOYSA-N

Opis

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.

Ta strona może zawierać tekst przetłumaczony maszynowo.

Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable