中文名称:

DYRK1B抑制剂(AZ191)

中文同义词:

DYRK1B抑制剂(AZ191);化合物AZ191

英文名称:

AZ191

英文同义词:

AZ-191;AZ 191;CS-1824;N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1h-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine;N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1h-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine, AZ191;[2-Methoxy-4-(4-methyl-piperazin-1-yl)-phenyl]-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-pyrimidin-2-yl]-amine;AZ191;2-Pyrimidinamine, N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-

CAS号:

1594092-37-1

分子式:

C24H27N7O

分子量:

429.52

EINECS号:

相关类别:

小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors

Mol文件:

1594092-37-1.mol

沸点 

705.3±70.0 °C(Predicted)

密度 

1.29±0.1 g/cm3(Predicted)

储存条件 

Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度 

DMSO: soluble10mg/mL, clear

形态

powder

酸度系数(pKa)

7.76±0.42(Predicted)

颜色

, white to yellow to light brown

生物活性

AZ191 是 DYRK1B 高效选择性抑制剂，IC50 值 17 nM。

靶点

IC50: 17 nM (DYRK1B)

体外研究

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.

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.

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.

WGK Germany 

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