847928-32-9
中文名稱
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
英文名稱
(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
2024/12/12 09:51:19
847928-32-9 結(jié)構(gòu)式
基本信息
中文別名
化合物 T14005 英文別名
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)-
物理化學(xué)性質(zhì)
沸點(diǎn)674.3±55.0 °C(Predicted)
密度1.304±0.06 g/cm3(Predicted)
儲(chǔ)存條件Keep in dark place,Sealed in dry,2-8°C
溶解度溶于DMSO(>20mg/ml)
酸度系數(shù)(pKa)7.25±0.33(Predicted)
形態(tài)固體
顏色米白色
穩(wěn)定性自購(gòu)買之日起 1 年內(nèi)保持穩(wěn)定。 DMSO 中的溶液可在 -20°C 下保存長(zhǎng)達(dá) 2 個(gè)月。
常見(jiàn)問(wèn)題列表
生物活性
1G244 是一種有效的 DPP8/9 抑制劑，IC50 分別為 12 nM 和 84 nM，但不抑制 DPPIV 和 DPPII。1G244 可誘導(dǎo)多發(fā)性骨髓瘤細(xì)胞凋亡，并具有抗骨髓瘤作用。靶點(diǎn)
IC50: 12 nM (DPP8), 84 nM (DPP9)
體外研究
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. |
體內(nèi)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. |