PSB-12379 ditriethylamine salt

PSB-12379 ditriethylamine salt 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)。

CAS号

T12569L

分子式

C30H53N7O9P2

主要靶点

CD73

仅限科研使用

Cat No : CM14656

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Synonyms



产品信息

PSB-12379 ditriethylamine salt, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).

CAS号 T12569L
分子式 C30H53N7O9P2
主要靶点 CD73
主要通路 免疫与炎症
分子量 717.73
纯度 98.26%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

体外活性

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].

溶解度

DMSO:11 mg/mL (15.33 mM)

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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