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 |
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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;JK184,刺猬信号抑制剂 |
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 |
结构式 |
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 性质
储存条件 | Keep in dark place,Inert atmosphere,2-8°C |
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溶解度 | 二甲基亚砜:≥20mg/mL |
形态 | 粉末 |
颜色 | 灰白色至浅棕色 |
Target | Value |
Gli
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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).
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.
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-13307 | 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 JK184 | 315703-52-7 | 5 mg | 450元 |
2024/08/19 | HY-13307 | 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 JK184 | 315703-52-7 | 10mM * 1mLin DMSO | 495元 |