NAMPT/IDO1-IN-1
Modify Date: 2024-01-16 20:31:11
NAMPT/IDO1-IN-1 structure
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Common Name | NAMPT/IDO1-IN-1 | ||
|---|---|---|---|---|
| CAS Number | 2247884-06-4 | Molecular Weight | 559.39 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H24BrFN8O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of NAMPT/IDO1-IN-1NAMPT/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]. |
| Name | NAMPT/IDO1-IN-1 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
IDO1:233 nM (IC50) NAMPT:57.7 nM (IC50) |
| 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]。 |
| 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]。 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. |
| References |
| Molecular Formula | C23H24BrFN8O3 |
|---|---|
| Molecular Weight | 559.39 |