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122110-53-6

中文名稱 (2,2-二甲基-1-氧代丙氧基)丁酸甲酯
CAS 122110-53-6
分子式 C10H18O4
分子量 202.25
MOL 文件 122110-53-6.mol
更新日期 2024/11/11 11:10:42
122110-53-6 結(jié)構(gòu)式 122110-53-6 結(jié)構(gòu)式

基本信息

中文別名
(2,2-二甲基-1-氧代丙氧基)丁酸甲酯
英文別名
Pivanex
Brn 4861411
pivalyloxymethyl butyrate
((2,2-Dimethylpropanoyl)oxy)methyl butanoate
Butanoic acid, (2,2-dimethyl-1-oxopropoxy)methyl ester

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C
溶解度二甲基亞砜:≥10mg/mL
形態(tài)oil
顏色無(wú)色或微黃色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H402-H315
防范說(shuō)明P273-P501
WGK Germanynwg

常見問題列表

生物活性
Pivanex (AN-9) 是丁酸的衍生物,是口服有效的 HDAC 抑制劑。Pivanex 可下調(diào) bcr-abl 蛋白,增強(qiáng)凋亡 (apoptosis)。Pivanex 具有抗轉(zhuǎn)移和抗血管生成的活性
靶點(diǎn)

HDAC

Bcr-Abl

體外研究

Pivanex (100-500 μM) exhibits significant anti-proliferation activity in K562 cells.
Pivanex (100-500 μM) also enhances apoptosis and caspase activity in K562 cells.
Pivanex (200 μM) induces enhancement in the G2-M phase, a moderate enhancement in the S phase and a slight reduction in G0-G1 of the cell cycle.
Pivanex (AN-9) has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines.

Cell Viability Assay

Cell Line: K562 cells.
Concentration: 100-500 μM.
Incubation Time: 24 hours.
Result: Reduced the number of K562 viable cells significantly.
100 μM Pivanex with 0.125 or 0.25 μM STI571 reduced the number of viable cells synergistically.

Apoptosis Analysis

Cell Line: K562 cells.
Concentration: 100-500 μM.
Incubation Time: 6-72 hours.
Result: Increased the number of K562 apoptotic cells significantly.
Increased the caspase activity in K562 cells significantly after only 4 h of incubation with 500 μM.
體內(nèi)研究

Pivanex (AN9, 200 mg/kg, b.i.d, daily) significantly improves the survival of SMN7 SMA mice. Pivanex (AN9) treatment also marked delays the end stage of disease as defined by the onset of body mass loss.

Animal Model: SMN7 SMA mice (SMN2 +/+ ; SMN7 +/+ ; mSmn ?/? ).
Dosage: 200 mg/kg.
Administration: Oral administration, b.i.d, at 09.00 and 17.00 daily.
Result: Improved the mean lifespan of treated SMN7 SMA mice by 84.6%.
Delayed the onset of body mass loss in SMN7 SMA mice by 94.9%.
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