1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO) NAMPT
  3. NAMPT/IDO1-IN-1

NAMPT/IDO1-IN-1 是一种口服有效的、靶向 NAMPTIDO1 的双抑制剂,IC50 分别为 57.5 nM 和 233 nM。NAMPT/IDO1-IN-1 阻断 NAD+ 的生物合成,抑制对紫杉醇 (HY-B0015) 和 FK866 (HY-50876) 耐药的 NSCLC 细胞系 (A549/R 细胞) 的增殖和迁移。NAMPT/IDO1-IN-1 在小鼠体内显示出抗肿瘤作用,并增强 A549/R 细胞对紫杉醇的敏感性。

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NAMPT/IDO1-IN-1 Chemical Structure

NAMPT/IDO1-IN-1 Chemical Structure

CAS No. : 2247884-06-4

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查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel[1].

IC50 & Target[1]

IDO1

233 nM (IC50)

NAMPT

57.7 nM (IC50)

体外研究
(In Vitro)

NAMPT/IDO1-IN-1 (化合物 10e) (10 μM; 48 h) 对 A549/R 细胞具有抗增殖活性,并依赖于 NAMPT 和 IDO1[1]
NAMPT/IDO1-IN-1 (5 μM, 10 μM, 15 μM; 12 d) 抑制 A549/R 细胞的集落形成,并以剂量依赖的方式促进细胞内 ROS 的积累[1]
NAMPT/IDO1-IN-1 (10 μM; 24 h) 以 NAMPT 和 IDO1 依赖的方式减少 A549/R 细胞中的 NAD+[1]

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

体内研究
(In Vivo)

NAMPT/IDO1-IN-1 (化合物 10e) (5 μM; 24 h) 对斑马鱼胚胎的 ROS 有促进作用,其 ROS 水平远高于 LPS (50 μg/mL) 处理[1]
NAMPT/IDO1-IN-1 (25 mg/kg; 口服; 单次剂量) 具有良好的口服生物利用度和 (5 mg/kg; 静脉注射; 单次剂量) 显示出中等整体暴露度[1]
NAMPT/IDO1-IN-1 (50、100、200 mg/kg; 口服; 每天 2 次, 共 3 周) 在 A549/R 肿瘤异种移植模型中也显示出体内抗肿瘤作用[1]

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

Animal Model: Female nude 6-8 week old mice with A549/R cells[1]
Dosage: 50, 100, and 200 mg/kg
Administration: Oral gavage; twice daily for 3 weeks
Result: Showed much better inhibitory activity against A549/R xenografts compared with the single agent.
Showed comparable anti-tumor efficacy with the combination of FK866 and epacadostat at dose of 100 mg/kg, while at 200 mg/kg showed better efficacy than the combination group.
分子量

559.39

Formula

C23H24BrFN8O3

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
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  • 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:
NAMPT/IDO1-IN-1
目录号:
HY-148572
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