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关于此项目
经验公式(希尔记法):
C20H20N4O6S
化学文摘社编号:
分子量:
444.46
UNSPSC Code:
41106305
MDL number:
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
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.
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存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable