847928-32-9
中文名称
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
英文名称
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
CAS
847928-32-9
分子式
C29H30F2N4O2
分子量
504.57
MOL 文件
847928-32-9.mol
更新日期
2025/02/13 15:05:43
847928-32-9 结构式
基本信息
中文别名
化合物 T14005 英文别名
1G244(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butaned
(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)-
物理化学性质
沸点674.3±55.0 °C(Predicted)
密度1.304±0.06 g/cm3(Predicted)
储存条件Keep in dark place,Sealed in dry,2-8°C
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。
常见问题列表
生物活性
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。靶点
IC50: 12 nM (DPP8), 84 nM (DPP9)
体外研究
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. |
体内研究
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. |