1. Immunology/Inflammation
  2. CD73
  3. CD73-IN-14

CD73-IN-14 是一种有效、选择性和具有口服活性的 CD73 抑制剂,IC50 值为 0.17 nM。CD73-IN-14 增加肿瘤浸润性 CD8+ 细胞数量并显示出抗肿瘤活性。CD73-IN-14 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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CD73-IN-14 Chemical Structure

CD73-IN-14 Chemical Structure

CAS No. : 2407356-67-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

D73-IN-14 is a potent, selective and orally active CD73 inhibitor with an IC50 value of 0.17 nM. CD73-IN-14 increases the number of tumor-infiltrating CD8+ cells and shows anti-tumor activity[1]. CD73-IN-14 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

C50: 0.17 nM (CD73)[1]

体内研究
(In Vivo)

CD73-IN-14 (10, 25, 50 mg/kg; p.o.; twice-a-day for 20 days) shows anti-tumor activity in mouse[1].br/> Pharmacokinetic Parameters of CD73-IN-14 in rats[1].

PO Dose (mg/kg) AUC0-24 h (ng*hr/mL) Cmax(nM) Tmax(hr)
50 580 74 0.8
200 6094 1800 0.8
500 18500 11000 0.3
rats, 50, 200, 500 mg/kg p.o.[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (EG7 model)[1]
Dosage: 10, 25, 50 mg/kg
Administration: P.o.; twice a day for 20 days
Result: Increased tumor-infiltrating CD8+ cells and decreased the tumor volume in a dose dependet manner.
分子量

615.98

Formula

C26H26ClN7O9

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

CD73-IN-14 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CD73-IN-14
目录号:
HY-152074
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