N-(4-乙氧基苯基)-4-(2-甲基咪唑并[1,2-A]吡啶-3-基)噻唑-2-胺

中文名称:

N-(4-乙氧基苯基)-4-(2-甲基咪唑并[1,2-A]吡啶-3-基)噻唑-2-胺

中文同义词:

N-(4-乙氧苯基)-4-(2-甲基咪唑并-[1,2-A]吡啶-3-基)噻唑-2-胺;N-(4-乙氧基苯基)-4-(2-甲基咪唑并[1,2-A]吡啶-3-基)噻唑-2-胺;HEDGEHOG(HH)抑制剂(JK184);化合物JK184

英文名称:

N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine

英文同义词:

N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine;Hh Signaling Antagonist VII, JK184;JK 184;N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-2-thiazolamine;2-ThiazolaMine, N-(4-ethoxyphenyl)-4-(2-MethyliMidazo[1,2-a]pyridin-3-yl)-;Hh Signaling Antagonist VII, JK184 - CAS 315703-52-7 - Calbiochem;CS-2369;JK184 (JK-184

CAS号:

315703-52-7

分子式:

C19H18N4OS

分子量:

350.44

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

315703-52-7.mol

储存条件 

Keep in dark place,Inert atmosphere,2-8°C

溶解度 

DMSO: ≥20mg/mL

形态

powder

颜色

off-white to light brown

生物活性

JK184抑制Hedgehog信号通路中的Gli，在哺乳动物细胞中IC50为30 nM。

靶点

Target Value Gli ()

Target

Value

Gli ()

体外研究

JK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcriptional activity in a dose dependent manner. JK184 significantly inhibitts proliferation of HUVECs with IC 50 of 6.3 μg/mL after three days incubation. To evaluate anti-tumor effect of JK184, MTT assay is conducted in Panc-1 and BxPC-3 cells after administration with indicated concentrations of compounds, half maximal inhibitory concentration (IC 50 ) of JK184 (23.7 ng/mL in anc-1 and 34.3 ng/mL in BxPC-3). Claudin-low cell lines are more sensitive to JK184 treatment than are MCF10a, MTSV1-7, or HMLE-shGFP and HMLE-pBP cells, and JK184 induced a dose-dependent decrease in glioma-associated oncogene homolog 1 ( GLI1 ) transcript and protein levels in these cells. Treatment with the IC 50 dose of JK184 enhances the proportion of HMLE-shEcad cells that stained with Annexin-V, but are negative for propidium iodide (PI) (P<0.0001, t test).

体内研究

JK184 (5 mg/kg, injected intravenously) exhibits good anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate as antitumor drug targeted Hh signaling. However, JK184 has a poor pharmacokinetic profile and bioavailability.

危险品标志 

Xn

危险类别码 

22-41

安全说明 

26-36

WGK Germany 

3