| 中文名 | JK184 |
| 英文名 | N-(4-ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-thiazol-2-amine |
| 别名 | 化合物JK184 HEDGEHOG(HH)抑制剂(JK184) 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 |
| 英文别名 | JK184 JK 184 CS-2369 JK184 (JK-184 Hh Signaling Antagonist VII, JK184 N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine 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)- N-(4-ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-thiazol-2-amine |
| CAS | 315703-52-7 |
| 化学式 | C19H18N4OS |
| 分子量 | 350.44 |
| 溶解度 | DMSO: ≥ 20 mg/mL |
| 存储条件 | Keep in dark place,Inert atmosphere,2-8°C |
| 外观 | 粉末 |
| 颜色 | off-white to light brown |
| MDL号 | MFCD01044465 |
| 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 - 有害物品![]() |
| 风险术语 | R22 - 吞食有害。 R41 - 对眼睛有严重伤害。 |
| 安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
| WGK Germany | 3 |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.853 ml | 14.267 ml | 28.535 ml |
| 5 mM | 0.571 ml | 2.853 ml | 5.707 ml |
| 10 mM | 0.285 ml | 1.427 ml | 2.853 ml |
| 5 mM | 0.057 ml | 0.285 ml | 0.571 ml |







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