杯苋甾酮

生物活性靶点体外研究体内研究杯苋甾酮试剂级价格

杯苋甾酮

CAS号:17086-76-9
英文名:Cyasterone
中文名:杯苋甾酮
CBNumber:CB9167302
分子式:C29H44O8
分子量:520.65
MOL File:17086-76-9.mol

杯苋甾酮化学性质

熔点 :164～166℃
沸点 :735.2±60.0 °C(Predicted)
密度 :1.31±0.1 g/cm3(Predicted)
储存条件 :under inert gas (nitrogen or Argon) at 2–8 °C
溶解度 :Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
形态 :Powder
酸度系数(pKa) :14.12±0.70(Predicted)
颜色 :White to off-white

安全信息

安全说明 :24/25
海关编码 :29322090

杯苋甾酮性质、用途与生产工艺

生物活性 Cyasterone，一种天然的 EGFR 抑制剂，主要分离自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通过诱导细胞凋亡 (apoptosis) 和细胞周期阻滞表现出抗增殖作用。 Cyasterone 可用于抗人类肿瘤的相关研究。
靶点

IC50: EGFR

体外研究

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.

体内研究

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.