1594092-37-1
中文名稱
DYRK1B抑制劑(AZ191)
英文名稱
AZ191
CAS
1594092-37-1
分子式
C24H27N7O
分子量
429.52
MOL 文件
1594092-37-1.mol
更新日期
2024/04/08 11:57:25
1594092-37-1 結(jié)構(gòu)式
基本信息
中文別名
化合物AZ191DYRK1B抑制劑(AZ191)
英文別名
AZ191CS-1824
AZ-191
AZ 191
N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1h-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine
2-Pyrimidinamine, N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-
[2-Methoxy-4-(4-methyl-piperazin-1-yl)-phenyl]-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-pyrimidin-2-yl]-amine
N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1h-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine, AZ191
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
沸點705.3±70.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度DMSO：可溶10mg/mL，澄清
酸度系數(shù)(pKa)7.76±0.42(Predicted)
形態(tài)粉末
顏色白色至黃色至淺棕色
常見問題列表
生物活性
AZ191 是 DYRK1B 高效選擇性抑制劑，IC50 值 17 nM。靶點
IC50: 17 nM (DYRK1B)
體外研究
AZ191 (0.01-60μM; 5 days) inhibits SW872 and SW982 cell lines in dose-dependent manner with IC
50
s of 3.183 μM and 1.279 μM, respectively.
AZ191 (1-5 μM; 48 hours) down-regulates three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations.
Cell Proliferation Assay
| Cell Line: | SW872, SW982 liposarcoma cells |
| Concentration: | 0.01, 0.03, 0.1, 0.3, 0.6, 1, 3, 6, 10, 20, 60 μM |
| Incubation Time: | 5 days |
| Result: | Dose-dependent growth inhibition with IC 50 s of 3.183 μM and 1.279 μM for SW872 and SW982 cell lines, respectively. |
Western Blot Analysis
| Cell Line: | SW872, SW982 liposarcoma cells |
| Concentration: | 1, 2, 3, 4, 5 μM |
| Incubation Time: | 48 hours |
| Result: | Down-regulated three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations. |