PSB-12379
目录号: PL01122 纯度: ≥99%
CAS No. :1802226-78-3
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中文名称
PSB-12379
中文别名
PSB-12379;化合物 T12569
英文名称
PSB-12379
英文别名
PSB-12379;N6-benzyl-(alpha,beta)-methylene-ADP;[[(2R,3S,4R,5R)-5-[6-(benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]methylphosphonic acid;BDBM50546335;(1-Deoxy-1-(6-benzylamino-9H-purine-9-yl)-beta-D-ribofuranose-5-O-yl)phosphonylmethylphosphonic acid;PSB-12379 disodium;Adenosine, N-(phenylmethyl)-, 5'-[hydrogen P-(phosphonomethyl)phosphonate]
Cas No.
1802226-78-3
分子式
C18H23N5O9P2
分子量
515.35
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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)。
生物活性
PSB-12379, a nucleotide analogue, is a potent Ecto-5-Nucleotidase (CD73) inhibitor with K i s of 9.03 nM (rat) and 2.21 nM (human).
性状
Solid
IC50 & Target[1][2]
Ki: 9.03 nM (rat), 2.21 nM (human) (Ecto-5’-Nucleotidase)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
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.
溶解度数据
In Vitro: H2O : 125 mg/mL (236.13 mM; Need ultrasonic)DMSO : ≥ 5 mg/mL (9.45 mM)
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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