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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
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- CAS号:
- 847928-32-9
- 英文名:
- (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
- 英文别名:
- 1G244;1G-244,1G244;(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)-
- 中文名:
- (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
- 中文别名:
- 化合物 T14005
- CBNumber:
- CB23367548
- 分子式:
- C29H30F2N4O2
- 分子量:
- 504.57
- MOL File:
- 847928-32-9.mol
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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione化学性质
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沸点:
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674.3±55.0 °C(Predicted)
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密度:
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1.304±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C(protect from light)
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溶解度:
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Soluble in DMSO (>20 mg/ml)
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酸度系数(pKa):
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7.25±0.33(Predicted)
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形态:
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solid
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颜色:
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Off-white
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稳定性:
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Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione性质、用途与生产工艺
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
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Cell Line:
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Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells
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Concentration:
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0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM
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Incubation Time:
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72 hours
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Result:
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Dose-dependently decreased viable cell number of five multiple myeloma cell lines.
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Western Blot Analysis
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Cell Line:
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MM.1 S cells
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Concentration:
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50 μM
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Incubation Time:
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0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours
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Result:
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Decreased caspase-3 and PARP protein.
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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.
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Animal Model:
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NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells
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Dosage:
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30 mg/kg
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Administration:
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Subcutaneous injection; once-a-week; for 3 weeks
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Result:
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Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.
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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 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 |
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
生产厂家
847928-32-9, (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione 相关搜索:
- 抑制剂
- 活性分子
- C29H30F2N4O2
- 化合物 T14005
- 847928-32-9
- 1G-244,1G244
- 2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butaned
- 1,4-Butanedione, 2-amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-, (2S)-
- (2S)-2-amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-(1,3-dihydroisoindol-2-yl)butane-1,4-dione
- 1G244
- (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione