氢溴酸卤夫酮
| 中文名称 | 氢溴酸卤夫酮 |
|---|---|
| 中文同义词 | 氢溴酸常山酮溶液, 100PPM;氢溴酸常山酮/哈洛夫酮;卤夫酮氢溴酸盐;-溴-6-氯-3-[3-(3-羟基-2-哌啶基)-2-丙酮基]-4(3H)-喹唑啉酮氢溴酸盐;7-溴-6-氯-3-[3-(3-羟基-2-哌啶基)-2-丙酮基]-4(3H)-喹唑啉酮氢溴酸盐;氢溴酸卤夫酮;氢溴酸溴氯哌喹酮;氢溴酸常山酮 |
| 英文名称 | Halofuginone hydrobromide |
| 英文同义词 | Ru-19110;Tempostatin;Unii-ptc2969mv1;rel-7-BroMo-6-chloro-3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3H)-quinazolinone HydrobroMide;trans-(+/-)-7-BroMo-6-chloro-3-[3-(3-hydroxy-2- piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone MonohydrobroMide;7-BroMo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one hydrobroMide;HALOFUGINONEHYDROBROMIDE;STENOROL |
| CAS号 | 64924-67-0 |
| 分子式 | C16H17BrClN3O3.HBr |
| 分子量 | 495.59 |
| EINECS号 | |
| 相关类别 | 其他兽药标准品;化工中间体;原料药;原料药;有机化工原料;标准品;Amines;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 64924-67-0.mol |
| 结构式 |  |
氢溴酸卤夫酮 性质
| 熔点 | 247° (dec) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 在DMSO中水中的溶解度为至100mM。 |
Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)
Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase.
The IC
50
s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC
50
s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC
50
of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively.
Cell Viability Assay
| Cell Line: | KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation |
| Concentration: | 1, 10, 100, 1000, 10000 nM |
| Incubation Time: | 48 hours |
| Result: | The IC 50 s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively. |
Western Blot Analysis
| Cell Line: | KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation |
| Concentration: | 1, 10, 100, 1000 nM |
| Incubation Time: | 24 hours |
| Result: | The IC 50 s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. |
Halofuginone (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage.
Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone.
| Animal Model: | 3-month-old male C57BL/6J (WT) mice |
| Dosage: | 0.2, 0.5, 1 or 2.5 mg/kg |
| Administration: | Injected intraperitoneally every other day for 1 month |
| Result: | Attenuated progression of OA in ACLT mice. |
| Animal Model: | Male nude mice (BALB/C nu/nu mice) (6-8-week) |
| Dosage: | 0.25 mg/kg |
| Administration: | Intraperitoneally injected; every day; 16 days |
| Result: | The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-N1584A | 氢溴酸卤夫酮 Halofuginone hydrobromide | 64924-67-0 | 5mg | 1200元 |
| 2024/01/25 | HY-N1584A | 氢溴酸卤夫酮 Halofuginone hydrobromide | 64924-67-0 | 10mM * 1mLin DMSO | 1320元 |