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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

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About This Item

Empirical Formula (Hill Notation):
C20H20N4O6S
CAS Number:
Molecular Weight:
444.46
UNSPSC Code:
41106305
MDL number:
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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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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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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