中文名 | 氢溴酸卤夫酮 |
英文名 | Halofuginone hydrobromide |
别名 | 氢溴酸常山酮 氢溴酸卤夫酮 卤夫酮氢溴酸盐 氢溴酸溴氯哌喹酮 氢溴酸常山酮|哈洛夫酮 氢溴酸常山酮溶液,100PPM 氢溴酸常山酮溶液, 100PPM -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 |
英文别名 | STENOROL Ru-19110 Tempostatin Unii-ptc2969mv1 HALOFUGINONEHYDROBROMIDE Halofuginone hydrobromide 7-BroMo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-onehydrobroMide 7-BroMo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one hydrobroMide rel-7-BroMo-6-chloro-3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3H)-quinazolinoneHydrobroMide rel-7-BroMo-6-chloro-3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3H)-quinazolinone HydrobroMide |
CAS | 64924-67-0 |
化学式 | C16H17BrClN3O3.HBr |
分子量 | 495.59 |
熔点 | 247° (dec) |
溶解度 | 在DMSO中可溶至100 mM。 |
存储条件 | Store at -20°C |
外观 | 整洁 |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xn - 有害物品 |
风险术语 | 22 - 吞食有害。 |
危险品运输编号 | UN2811 - class 6.1 - PG 1 - EHS - Toxic solids, organic, n.o.s., HI: all |
WGK Germany | 3 |
RTECS | VA2397066 |
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