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2241014-82-2

中文名称 NAMPT inhibitor-linker 2
英文名称 NAMPT inhibitor-linker 2
CAS 2241014-82-2
分子式 C34H33FN6O5
分子量 624.66
MOL 文件 2241014-82-2.mol
2241014-82-2 结构式 2241014-82-2 结构式

基本信息

中文别名
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
英文别名
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]-

物理化学性质

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Solid
颜色Off-white to light yellow
NAMPT inhibitor-linker 2价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/12/22HY-112616NAMPT inhibitor-linker 22241014-82-21 mg1364元
2025/12/22HY-112616NAMPT inhibitor-linker 22241014-82-25 mg3000元
2025/12/22HY-112616NAMPT inhibitor-linker 22241014-82-210 mg4800元

常见问题列表

生物活性
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。
靶点

Traditional Cytotoxic Agents

体外研究

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.
体内研究

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.
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