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17086-76-9

中文名稱 杯莧甾酮
英文名稱 Cyasterone
CAS 17086-76-9
分子式 C29H44O8
分子量 520.65
MOL 文件 17086-76-9.mol
更新日期 2025/01/25 09:07:49
17086-76-9 結(jié)構(gòu)式 17086-76-9 結(jié)構(gòu)式

基本信息

中文別名
杯覓甾酮
杯莧甾酮
杯莧甾酮(標(biāo)準(zhǔn)品)
杯莧甾酮(杯覓甾酮)
杯莧甾酮, 來源于川牛膝
CYASTERONE 杯莧甾酮
英文別名
cyasteron
CYASTERONE
(22r,24s,25s,28r)-gamma-lacton
Cyasterone, 98%, from Cyathula officinalis K.C. Kuan
2-beta,3-beta,14,20,22,28-hexahydroxy-6-oxo-5-beta-stigmast-7-en-26-oicaci
(22R,24S,25S,28R)-2β,3β,14,20,22,28-Hexahydroxy-6-oxo(26-13C)-5β-stigmasta-7-ene-26-oic acid γ-lactone
7,(5BETA)-CHOLESTEN-26-CARBOXYLIC ACID-24BETA-(1-HYDROXYETHYL)-2BETA, 3BETA, 14ALPHA,20BETA, 22R-PENTOL-6-ONE GAMMA-LACTONE
(3S,4S,5R)-4-[(2R,3R)-2,3-Dihydroxy-3-[(2S,3R,5R,9R,10R,13R,14S,17S)-2,3,14-trihydroxy-10,13-dimethyl-6-oxo-2,3,4,5,9,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-17-yl]butyl]-3,5-dimethyloxolan-2-one
所屬類別
生物化工:提取物

物理化學(xué)性質(zhì)

外觀性狀白色結(jié)晶,溶于甲醇、乙醇、DMSO,來源于川牛膝CyathulaofficinalisKuan的干燥根。
熔點(diǎn)164~166℃
沸點(diǎn)735.2±60.0 °C(Predicted)
密度1.31±0.1 g/cm3(Predicted)
儲(chǔ)存條件Keep in dark place,Inert atmosphere,2-8°C
溶解度Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
酸度系數(shù)(pKa)14.12±0.70(Predicted)
形態(tài)粉末
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS05,GHS02
警示詞危險(xiǎn)
危險(xiǎn)性描述H314-H226
安全說明24/25
海關(guān)編碼29322090

應(yīng)用領(lǐng)域

用途1
用于含量測(cè)定/鑒定/藥理實(shí)驗(yàn)等。
藥理藥效:養(yǎng)血舒筋, 祛風(fēng)除濕。
用途2
杯莧甾酮有抗生育,活血,利膽,降脂的作用。

常見問題列表

生物活性
Cyasterone,一種天然的 EGFR 抑制劑,主要分離自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通過誘導(dǎo)細(xì)胞凋亡 (apoptosis) 和細(xì)胞周期阻滯表現(xiàn)出抗增殖作用。 Cyasterone 可用于抗人類腫瘤的相關(guān)研究。
靶點(diǎn)

IC50: EGFR

體外研究

Cyasterone exerts cytotoxicity on multiple cell lines: HeLa (IC 50 =77.24 μg/ml); HepG-2 (IC 50 =52.03 μg/ml); MCF-7 (IC 50 =82.07 μg/ml) and MCF-7 (IC 50 =82.07 μg/ml). And It has none cytotoxicity (IC 50 >400 μg/ml) on 3 types of carcinoma (HT-29, Caco-2, T47D) and 1 type of normal (NIH 3T3) cell lines. Cyasterone (0-60 μg/ml; 48 hours) causes a significantly decreasing of the cell proliferation. It inhibits cell growth as a dose-dependent manner, exhibits IC 50 values of 38.50 μg/ml and 32.96 μg/ml, respectively. Cyasterone (0-60 μg/ml; 24 hours) decreases p-EGFR, p-MEK, and p-mTOR as a dose-dependent manner in A549 cells, it affects the MAPK signaling pathway activities.

Cell Viability Assay

Cell Line: A549 cells and MGC823 cells
Concentration: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
Incubation Time: 24 hours
Result: Inhibited cell proliferation as a dose-dependent manner.

Western Blot Analysis

Cell Line: A549 cells
Concentration: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
Incubation Time: 24 hours
Result: Surpressed p-EGFR, p-MEK, and p-mTOR expression.
體內(nèi)研究

Cyasterone (intraperitoneal injection; 5 mg/kg, 10 mg/kg and 15 mg/kg; 21 days) has anti-proliferation effect in vivo and inhibits MGC823 cells xenografted tumor growth in vivo with few changes in body weights.

Animal Model: MGC823 xenograft tumor in BALB/C-nu mice
Dosage: 5 mg/kg, 10 mg/kg and 15 mg/kg
Administration: Intraperitoneal injection
Result: Inhibited MGC823 xenograft tumor growth in vivo.
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