Subasumstat
(Synonyms: TAK-981) 目录号 : GC64972An inhibitor of SUMO-activating enzyme
Cas No.:1858276-04-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
TAK-981 is an inhibitor of SUMO-activating enzyme (SAE; IC50 = <10 nM).1 It increases macrophage phagocytosis and natural killer (NK) cell-mediated cytotoxicity of cancer cells in vitro.2 TAK-981 upregulates the expression of IFN-regulated genes in the blood and tumor tissue in an A20 syngeneic lymphoma mouse model.3 It also decreases intratumor levels of SUMOlyated proteins and reduces tumor growth in the same model.
1.Duffey, M.O., England, D., Freeze, S., et al.Heteroaryl compounds useful as inhibitors of sumo activating enzymeWO2016/004136 Al(2016) 2.Nakamura, A., Grossman, S., Song, K., et al.Abstract 1523: Inhibition of SUMOylation by TAK-981 induces antitumor innate immune responses by modulating macrophage and NK cell function through Type I IFN pathway activationCancer Res.79(13)1523(2019) 3.Berger, A.J., Friedlander, S., Ghasemi, O., et al.Abstract 3079: Pharmacodynamic evaluation of the novel SUMOylation inhibitor TAK-981 in a mouse tumor modelCancer Res.79(13)3079(2019)
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.7298 mL | 8.649 mL | 17.298 mL |
5 mM | 0.346 mL | 1.7298 mL | 3.4596 mL |
10 mM | 0.173 mL | 0.8649 mL | 1.7298 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。