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首页-抗体药物偶连体和PROTACs-PROTAC-CQ627
CQ627

Chemical Structure : CQ627

CAS No.:

CQ627 (CQ-627)

货号: PC-23702Not For Human Use, Lab Use Only.

CQ627 is the first right open reading frame kinase 2 (RIOK2) molecular glue degrader with DC50 value of 410 nM and Dmax of 83.4% in MOLT4 leukemia cell line via UPS by recruiting E3 ubiquitin ligase RNF126.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CQ627 is the first right open reading frame kinase 2 (RIOK2) molecular glue degrader with DC50 value of 410 nM and Dmax of 83.4% in MOLT4 leukemia cell line via UPS by recruiting E3 ubiquitin ligase RNF126.
CQ627 (1 uM) significantly down-regulated RIOK2 protein level at 12 h, with a maximum degradation of 94.8 % at 24 h.
CQ627 dose-dependently induces apoptosis and blocks cell cycles in G2/M phase in MOLT4 leukemia cells.
CQ627 suppresses ATPase activity (IC50=98.42 nM) and downstream signal of RIOK2. CQ627 induces MOLT-4 cell cycle arrest and apoptosis.
CQ627 displays potent antiproliferative activity in various tumor cells, with superior activity (IC50 < 0.35 μM) in MOLT-4, HL-60 and OCILY3 cell lines.
CQ627 (10 mg/kg, i.p.) inhibits tumor growth in the MOLT-4 tumor xenografted model.

物理化学性质&存储条件

分子量 697.65
分子式 C36H27F4N7O4
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

(E)-1-(4-fluorophenyl)-4-(4-(4-(8-(6-methoxypyridin-3-yl)-4-oxo-4,5-dihydro-1H-[1,2,3]triazolo[4,5-c]quinolin-1-yl)-2-(trifluoromethyl)phenyl)piperazin-1-yl)but-2-ene-1,4-dione

参考文献

1. Ma H, et al. Eur J Med Chem. 2024 Dec 15;283:117166.

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