NAMPT inhibitor-linker 2
| 中文名称 | NAMPT inhibitor-linker 2 |
|---|---|
| 中文同义词 | 4-(4-(3-(2,5-二氧代-2,5-二氢-1H-吡咯-1-基)丙酰基)哌嗪-1-基)-N-(2-氟-4-((1S,2S)-2-(吡啶-3-基)环丙烷-1-甲酰胺基)苄基)苯甲酰胺;化合物 NAMPT inhibitor-linker 2 |
| 英文名称 | NAMPT inhibitor-linker 2 |
| 英文同义词 | NAMPT inhibitor-linker 2;Benzamide, 4-[4-[3-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxopropyl]-1-piperazinyl]-N-[[2-fluoro-4-[[[(1S,2S)-2-(3-pyridinyl)cyclopropyl]carbonyl]amino]phenyl]methyl]- |
| CAS号 | 2241014-82-2 |
| 分子式 | C34H33FN6O5 |
| 分子量 | 624.66 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2241014-82-2.mol |
| 结构式 |  |
NAMPT inhibitor-linker 2 性质
| 沸点 | 940.2±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.395±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 13.91±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色至浅黄色 |
NAMPT inhibitor-linker 2 为 ADC 的一部分，由一种 NAMPT 的抑制剂作为有效载荷和一个连接物组成。ADC-4 由一个 NAMPT inhibitor-linker 2 和一个 anti-c-Kit 单克隆抗体组成，对表达 c-Kit 的细胞具有抑制作用，比如 GIST-T1 和 NCI-H526 细胞，IC50 值分别为 <7 pM 和 40 pM。
|
Traditional Cytotoxic Agents
|
ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC
50
s of <7 pM and 40 pM, respectively.
ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle.
Cell Proliferation Assay
| Cell Line: | GIST-T1 cells |
| Concentration: | 0.1 pM-10 nM |
| Incubation Time: | 144 hours |
| Result: | Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM. |
ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells.
| Animal Model: | Female scid-beige (SCID bg) mice |
| Dosage: | 20 mg/kg |
| Administration: | A single intravenous injection (i.v.) for 28 days |
| Result: | Significantly inhibited the growth of tumor in mice. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-112616 | NAMPT inhibitor-linker 2 | 2241014-82-2 | 1 mg | 1364元 |
| 2026/09/15 | HY-112616 | NAMPT inhibitor-linker 2 | 2241014-82-2 | 5 mg | 3000元 |