(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
生物活性靶点体外研究体内研究 用途与合成方法 MSDS (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione价格(试剂级) 上下游产品信息
| 中文名称 | (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione |
|---|---|
| 中文同义词 | 化合物 T14005 |
| 英文名称 | (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione |
| 英文同义词 | (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione;1G244;(2S)-2-amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-(1,3-dihydroisoindol-2-yl)butane-1,4-dione;1,4-Butanedione, 2-amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-, (2S)-;2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butaned;1G-244,1G244 |
| CAS号 | 847928-32-9 |
| 分子式 | C29H30F2N4O2 |
| 分子量 | 504.57 |
| EINECS号 | |
| 相关类别 | 活性分子 |
| Mol文件 | 847928-32-9.mol |
| 结构式 |  |
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 性质
| 沸点 | 674.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.304±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C(protect from light) |
| 溶解度 | 溶于DMSO(>20mg/ml) |
| 酸度系数(pKa) | 7.25±0.33(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色 |
| 稳定性 | 自购买之日起 1 年内保持稳定。 DMSO 中的溶液可在 -20°C 下保存长达 2 个月。 |
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 用途与合成方法
1G244 是一种有效的 DPP8/9 抑制剂，IC50 分别为 12 nM 和 84 nM，但不抑制 DPPIV 和 DPPII。1G244 可诱导多发性骨髓瘤细胞凋亡，并具有抗骨髓瘤作用。
IC50: 12 nM (DPP8), 84 nM (DPP9)
1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines.
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected.
Cell Viability Assay
| Cell Line: | Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells |
| Concentration: | 0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM |
| Incubation Time: | 72 hours |
| Result: | Dose-dependently decreased viable cell number of five multiple myeloma cell lines. |
Western Blot Analysis
| Cell Line: | MM.1 S cells |
| Concentration: | 50 μM |
| Incubation Time: | 0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours |
| Result: | Decreased caspase-3 and PARP protein. |
1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model.
| Animal Model: | NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells |
| Dosage: | 30 mg/kg |
| Administration: | Subcutaneous injection; once-a-week; for 3 weeks |
| Result: | Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-116304 | 1G244 | 1 mg | 318元 | |
| 2024/04/30 | HY-116304 | (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 1G244 | 847928-32-9 | 5mg | 700元 |