ATN-224

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Chemical Structure| 649749-10-0 同义名 : Bis(choline)tetrathiomolybdate; ALXN1840; Decuprate; Bis-choline tetrathiomolybdate
CAS号 : 649749-10-0
货号 : A252851
分子式 : C10H28MoN2O2S4
纯度 : 98%+
分子量 : 432.54
MDL号 : MFCD25976790
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 ATN-224 demonstrates a unique and robust attraction to copper ions (108 mol/L), without affinity for calcium, iron, magnesium, zinc, or manganese ions up to concentrations of 1 mM, as revealed by isothermal titration calorimetry. It restricts the growth of HUVEC (IC50=1.4±0.3 μM; n=5) and inhibits bovine SOD1 activity (IC50=0.33±0.03 μM after 24 hours). The suppression of SOD1 by ATN-224 is both time-bound, peaking around 16 hours, and dose-dependent, demonstrating an IC50 of 17.5±3.7 nM in endothelial cells. Additionally, it deters FGF-2-stimulated ERK1/2 phosphorylation correlating with its anti-proliferative IC50 range (1.25-2.5 μM)[1]. Orally administered ATN-224 targets and inhibits the copper/zinc-dependent superoxide dismutase 1 (Cu/Zn-SOD1) in endothelial and cancer cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

参考文献

[1]Juarez JC, et al. Copper binding by tetrathiomolybdate attenuates angiogenesis and tumor cell proliferation through the inhibition of superoxide dismutase 1. Clin Cancer Res. 2006 Aug 15;12(16):4974-82.

[2]Lin J, et al. A non-comparative randomized phase II study of 2 doses of ATN-224, a copper/zinc superoxide dismutase inhibitor, in patients with biochemically recurrent hormone-na?ve prostate cancer. Urol Oncol. 2013 Jul;31(5):581-8.