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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-FX1-5303
FX1-5303

Chemical Structure : FX1-5303

CAS No.: 2817633-13-7

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FX1-5303 (FX 1-5303)

货号: PC-22260Not For Human Use, Lab Use Only.

FX1-5303 is a highly potent, specific ubiquitin-specific protease 7 (USP7) inhibitor with biochemical IC50 of 0.29 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FX1-5303 is a highly potent, specific ubiquitin-specific protease 7 (USP7) inhibitor with biochemical IC50 of 0.29 nM.
FX1-5303 displays cellular potency by measuring the p53 accumulation with EC50 of 5.6 nM, inhibition of cell viability with IC50 of 15 nM in MM.1S multiple myeloma (MM) cell line, which is previously shown to be sensitive to USP7 inhibitors.
FX1-5303 is highly selective for USP7, does not inhibit a panel of 44 DUBs.
FX1-5303 (0-3 uM) induces a modest and transient increase of p53 in MRC5 cells.
FX1-5303 demonstrates potent antiproliferative activity in TP53 WT AML cell lines, including MV4-11 and OCI-AML-3, but lacks significant activity in the TP53 mutant HL-60 cell line.
FX1-5303 is synergistic with the BCL2 inhibitor venetoclax.
FX1-5303 (30 mg/kg and 40 mg/kg, BID) efficacious in vivo in mouse cell-line-derived xenograft models of multiple myeloma and acute myeloid leukemia.

物理化学性质&存储条件

分子量 521.08
分子式 C28H29ClN4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-1-((7-(6-chloro-1-(5-azaspiro[3.4]octan-7-yl)-1,2,3,4-tetrahydroquinolin-8-yl)thieno[3,2-b]pyridin-2-yl)methyl)pyrrolidine-2,5-dione

参考文献

1. Alan S Futran, et al. iScience. 2024 Apr 9;27(5):109693.

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