159989-64-7
基本信息
尼非那韦
娜芙维亚
萘非那韦
奈非那韦杂质
甲磺酸萘非那韦
2-[(2R,3R)-2-羟基-3-[(3-羟基-2-甲基苯甲酰)氨基]-4-(苯基硫)丁基]-(3S,4aS,8aS)-N-叔丁基十氢异喹啉-3-甲酰胺
nefinavir
NELFINAVIR
NELFINAVIR-12
8a-beta))-a-bet
NELFINAVIR USP/EP/BP
Nelfinavir Regeoisomer
AG 1341
AG-1341
AG1341
Nelfinavir & Nelfinavir Mesylate
3-isoquinolinecarboxamide,n-(1,1-dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hy
物理化学性质
熔点 | 185-186 °C |
比旋光度 | D -119.23° (c = 0.26 in methanol) |
沸点 | 786.8±60.0 °C(Predicted) |
密度 | 1.22±0.1 g/cm3(Predicted) |
储存条件 | Keep in dark place,Inert atmosphere,2-8°C |
溶解度 | ≥ 20.45mg/mL in Ethanol |
酸度系数(pKa) | pKa1 6.0; pKa2 11.06(at 25℃) |
形态 | Powder |
颜色 | White to off-white |
水溶解性 | 7g/L(temperature not stated) |
安全数据
危险性符号(GHS) | GHS07 |
警示词 | 警告 |
危险性描述 | H302 |
防范说明 | P501-P270-P264-P301+P312+P330 |
毒性 | rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998. |
常见问题列表
HIV-1
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Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells.
Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells.
Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines.
Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT.
Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system.
Cell Proliferation Assay
Cell Line: | RPMI, LP1, U266, OPM2 and MM1S cells |
Concentration: | 1, 2, 5, 10 μM |
Incubation Time: | 48 hours |
Result: | Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC 50 of 1-5 μM. |
Apoptosis Analysis
Cell Line: | LP1 and U266 cells |
Concentration: | 1-10 μM |
Incubation Time: | 17 hours |
Result: | Induced a dose-dependent increase in the percentage of annexin V + /propidium iodide + cells. |
Western Blot Analysis
Cell Line: | U266 cells |
Concentration: | 5 μM |
Incubation Time: | 0-24 hours |
Result: | The level of AKT phosphorylation in U266 cells decreased. |
Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice.
Animal Model: | NOD/SCID mice (bearing U266-luc cells) |
Dosage: | 75 mg/kg |
Administration: | I.p.; 5 days a week for 21 days |
Result: | Decreased MM cell growth in NOD/SCID mice. |