SML4057
PF-9363
≥98% (HPLC)
别名:
2,6-Dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]benzenesulfonamide, CTx 648, CTx-648, CTx648, PF9363
相关类别
生化/生理作用
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer
Cell Chemical Biology, 30(10) (2023)
Leslie Duplaquet et al.
Nature cell biology, 25(9), 1346-1358 (2023-08-18)
Small cell lung cancer (SCLC) exists broadly in four molecular subtypes: ASCL1, NEUROD1, POU2F3 and Inflammatory. Initially, SCLC subtypes were thought to be mutually exclusive, but recent evidence shows intra-tumoural subtype heterogeneity and plasticity between subtypes. Here, using a CRISPR-based
Timothy R Bishop et al.
Nature chemical biology, 19(10), 1215-1222 (2023-05-02)
Histone acetyltransferases (HATs) are implicated as both oncogene and nononcogene dependencies in diverse human cancers. Acetyl-CoA-competitive HAT inhibitors have emerged as potential cancer therapeutics and the first clinical trial for this class of drugs is ongoing (NCT04606446). Despite these developments
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