U104 是 CA IX 和 CA XII 碳酸酐酶 (CA) 抑制剂，其Ki分别为 45.1 nM 和 4.5 nM。小鼠模型中，它能够表现出明显的抑制肿瘤生长的作用。

U-104 is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

在4T1实验用转移小鼠模型中,U-104（19 mg/kg）可抑制转移形成.植入MDA-MB-231 LM2-4Luc+细胞的小鼠中, U-104（38 mg/kg）抑制原代肿瘤的生长并减少癌症干细胞数量.植入4T1细胞的Balb/c小鼠中,口服给药U-104（5 mg/mL）减缓了肿瘤生长速度.

在转移性MDA-MB-231LM2-4Luc +细胞中,U-104（<50 μM）以剂量依赖性方式显着降低细胞迁移。

Kinase assay: Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument.

178606-66-1

C13H12FN3O3S

309.32

MST-104;NSC-213841

DMSO:30.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years