亚美克松
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- CAS号:
- 59643-91-3
- 英文名:
- Imexon
- 英文别名:
- imexon;bm06002;AMpliMexon;Imexon
(Amplimexon;4-IMINO-1,3-DIAZABICYCLO-[3.1.0]HEXAN-2-ONE;4-Amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one;1,3-Diazabicyclo[3.1.0]hex-3-en-2-one, 4-amino-
- 中文名:
- 亚美克松
- 中文别名:
- 伊美克;亚美克松;亚胺氮环己酮;化合物 T15566;4-亚氨基-1,3-二氮杂双环[3.1.0]己-2-酮
- CBNumber:
- CB5274628
- 分子式:
- C4H5N3O
- 分子量:
- 111.1
- MOL File:
- 59643-91-3.mol
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亚美克松化学性质
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沸点:
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231.6±23.0 °C(Predicted)
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密度:
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2.26±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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4.79±0.20(Predicted)
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形态:
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Solid
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颜色:
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White to off-white
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亚美克松性质、用途与生产工艺
Imexon (BM 06002) 是一种氮杂环丙烷类化合物,具有抗癌的功效。
Imexon (BM 06002) induces oxidative stress in the ER, activates an ER stress response. Imexon (BM 06002) does not significantly alter the levels of eIF2B5, however there is a dose-dependent increase in the phosphorylation of eIF2alpha, as well as an increase in the levels of GTP exchange protein eIF2B2 in MiaPaCa-2, Panc-1, and BxPC3 cells. Imexon (BM 06002) induces single-stranded breaks in the human A375 melanoma cells but only significantly at the highest concentrations for each agent compared to controls. Imexon plus DTIC cytotoxicity is additive. Imexon (BM 06002) show inhibitory activities against MiaPaCa-2, Panc-1 and BxPC3, with IC
50
s of 275.5 ± 54.2, 147.4 ± 4.7 and 355.7 ± 114.7 μM.
Imexon (BM 06002) in combination with DTIC results in an increase in the peak plasma imexon level in non-tumor-bearing mice. The combination of both drugs increases plasma imexon AUC by 22% (p=0.026). Imexon (BM 06002) (100 mg/kg/day, i.v.) treatment decreases the body weight of SCID mice bearing human A375 melanoma tumors, but there is no significant difference in tumor growth. Imexon (BM 06002) (100 mg/kg) in combination with GEM shows synergistic inhibition of Panc-1 tumor growth in SCID mice.
亚美克松
上下游产品信息
上游原料
下游产品
59643-91-3, 亚美克松 相关搜索:
- 抑制剂
- 化合物 T15566
- 4-亚氨基-1,3-二氮杂双环[3.1.0]己-2-酮
- 伊美克
- 亚美克松
- 亚胺氮环己酮
- 59643-91-3
- 1,3-Diazabicyclo[3.1.0]hex-3-en-2-one, 4-amino-
- Imexon
(Amplimexon
- AMpliMexon
- 4-Amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one
- imexon
- 4-IMINO-1,3-DIAZABICYCLO-[3.1.0]HEXAN-2-ONE
- bm06002