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131436-22-1

中文名稱 尾孢素酰胺
英文名稱 Cercosporamide
CAS 131436-22-1
分子式 C16H13NO7
分子量 331.28
MOL 文件 131436-22-1.mol
131436-22-1 結構式 131436-22-1 結構式

基本信息

中文別名
尾孢素酰胺
英文別名
Cercosporamide
(-)-CERCOSPORAMIDE
4-Dibenzofurancarboxamide
Cercosporamide ((-)-Cercosporamide)
Cercosporamide from Cercosporidium henningsii
(R)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9aβ-methyl-9-oxodibenzofuran-4-carboxamide
(9aS)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-4-dibenzofurancaboxamide
4-Dibenzofurancarboxamide, 8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (9aS)-

物理化學性質(zhì)

沸點582.5±50.0 °C(Predicted)
密度1.70±0.1 g/cm3(Predicted)
儲存條件-20°C
溶解度氯仿:可溶1mg/mL
酸度系數(shù)(pKa)11.89±0.70(Predicted)
形態(tài)粉末
顏色White to yellow

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302
危險品標志Xn
危險類別碼22
WGK Germany3
海關編碼2934999090
尾孢素酰胺價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-16982尾孢素酰胺
Cercosporamide
131436-22-1500μg9500元
2023/10/26HY-16982尾孢素酰胺
Cercosporamide
131436-22-11mg16000元

常見問題列表

生物活性
Cercosporamide 是一種高效的 ATP 競爭性 Pkc1 激酶抑制劑,IC50 sub><50 nM,Ki<7 nM。Cercosporamide 是一種獨特的 Mnk 抑制劑。
靶點

Pkc1

50 nM (IC 50 )

Pkc1

7 nM (Ki)

Mnk

體外研究

Cercosporamide is a broad-spectrum natural antifungal compound, is actually a selective and highly potent fungal Pkc1 kinase inhibitor. Cercosporamide, an antifungal agent that is recently shown to act as a unique Mnk inhibitor, exhibits antileukemic properties. Cercosporamide is a potent inhibitor of phosphorylation of eIF4E at Ser209 in AML cells and results in potent inhibitory effects on primitive leukemic progenitors (CFU-L) from AML patients. To determine whether Cercosporamide exhibits negative regulatory effects on cell proliferation and viability of leukemia cells, MTT assays are conducted. When U937 cells are incubated in the presence or absence of the increasing doses of Cercosporamide, a dose-dependent suppression of cell growth is found. Similar experiments with comparable results are seen when the effects of Cercosporamide on MM6 and K562 cells are examined.

體內(nèi)研究

Treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (P<0.011 for 10 mg/kg twice-daily Cercosporamide; P<0.006 for Cercosporamide 20 mg/kg daily; P<0.0374 for Ara-C). The combination of Cercosporamide 10 mg/kg twice daily plus Ara-C is significantly more effective than either agent alone (P<0.0009 vs Cercosporamide; P=0.005 vs Ara-C; P<0.0001 vs either vehicle). Cercosporamide (20 mg/kg once daily) in combination with Ara-C shows similar effects, with significant inhibition of tumor growth vs captisol (P<0.0001) or water (P=0.0003), but does not show statistical significance vs Cercosporamide alone (20 mg/kg) or Ara-C alone.

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