PSB-12379

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PSB-12379  纯度: 99.54%

PSB-12379 是一种核苷酸类似物，是一种有效的 Ecto-5′-Nucleotidase (CD73) 抑制剂，Kis 值为 9.03 nM (鼠) 和 2.21 nM (人)。

PSB-12379

PSB-12379 Chemical Structure

CAS No. : 1802226-78-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in Water ￥2097 In-stock
5 mg ￥1850 In-stock
10 mg ￥2850 In-stock
25 mg ￥6300 In-stock
50 mg   询价  
100 mg   询价  

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PSB-12379 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Nucleotide Compound Library
  • Targeted Diversity Library

生物活性

PSB-12379, a nucleotide analogue, is a potent Ecto-5′-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human)[1][2].

IC50 & Target

Ki: 9.03 nM (rat), 2.21 nM (human) (Ecto-5’-Nucleotidase)[1]
体外研究
(In Vitro)

Metabolism: Only a small percentage (<23%) of PSB-12379 (10g) is metabolized under the applied conditions, while >77% of the compounds are recovered unchanged after a long incubation for 8 h. PSB-12379 (10g) is somewhat less stable, and 56% are metabolized within 8 h. Hydrolytic cleavage of the glycosidic bond, which is a typical phase I reaction of nucleosides and nucleotides, was observed as the main reaction[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

515.35

Formula

C18H23N5O9P2
CAS 号

1802226-78-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 125 mg/mL (242.55 mM; Need ultrasonic)

DMSO : ≥ 5 mg/mL (9.70 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9404 mL 9.7021 mL 19.4043 mL
5 mM 0.3881 mL 1.9404 mL 3.8809 mL
10 mM 0.1940 mL 0.9702 mL 1.9404 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Bhattarai S, et al. α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5′-Nucleotidase (CD73) Inhibitors. J Med Chem. 2015 Aug 13;58(15):6248-63.

    [2]. X-Ray Co-Crystal Structure Guides the Way to Subnanomolar Competitive Ecto-5 -Nucleotidase (CD73) Inhibitors for Cancer Immunotherapy Sanjay Bhattarai. Adv. Therap. 2019, 2, 1900075.

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