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64924-67-0

中文名称 氢溴酸卤夫酮
英文名称 Halofuginone hydrobromide
CAS 64924-67-0
分子式 C16H17BrClN3O3.HBr
分子量 495.59
MOL 文件 64924-67-0.mol
更新日期 2024/05/16 11:48:13
64924-67-0 结构式 64924-67-0 结构式

基本信息

中文别名
氢溴酸常山酮
氢溴酸卤夫酮
常山酮溴酸盐
卤夫酮氢溴酸盐
卤夫酮溴氢酸盐
氢溴酸溴氯哌喹酮
反式常山酮氢溴酸盐
氢溴酸卤夫酮 标准品
氢溴酸常山酮/哈洛夫酮
常山酮氢溴酸盐(消旋体)
英文别名
STENOROL
Ru-19110
Tempostatin
RU-19110(HBr)
Unii-ptc2969mv1
55837-20-2 (free)
RU-19110 (hydrobromide)
HALOFUGINONEHYDROBROMIDE
Trans-halofuginone hydrobromide
Halofuginone Hydrobromide 64924-67-0
所属类别
分析化学:分析标准品

物理化学性质

熔点247° (dec)
储存条件-20°C储存
溶解度在DMSO中水中的溶解度为至100mM。
形态neat

安全数据

危险性符号(GHS)
GHS06,GHS09
警示词危险
危险品标志Xn
危险类别码22
危险品运输编号UN2811 - class 6.1 - PG 1 - EHS - Toxic solids, organic, n.o.s., HI: all
WGK Germany3
RTECS号VA2397066
氢溴酸卤夫酮价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-N1584A氢溴酸卤夫酮
Halofuginone hydrobromide
64924-67-05mg1200元
2024/04/30HY-N1584A氢溴酸卤夫酮
Halofuginone hydrobromide
64924-67-010mM * 1mLin DMSO1320元
2024/04/30HY-N1584A氢溴酸卤夫酮
Halofuginone hydrobromide
64924-67-010mg1900元

常见问题列表

生物活性
Halofuginone hydrobromide (RU-19110 hydrobromide) 是 Febrifugine 的一种低毒性衍生物,可从 Dichroa febrifuga 中分离出来。Halofuginone 是一种 ATP 竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂,Ki 为 18.3 nM。Halofuginone 是 I 型胶原 (type-I collagen) 合成的特异性抑制剂,并通过抑制 TGF-β 活性可减轻骨关节炎。
靶点

Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)

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.
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