普林贝瑞

生物活性靶点体外研究体内研究普林贝瑞试剂级价格

普林贝瑞

CAS号:524684-52-4
英文名:Prinaberel
中文名:普林贝瑞
CBNumber:CB21509128
分子式:C15H10FNO3
分子量:271.24
MOL File:524684-52-4.mol

普林贝瑞化学性质

熔点 :250-252 ºC
沸点 :451.6±45.0 °C(Predicted)
密度 :1.413
储存条件 :room temp
溶解度 :DMSO: ≥25mg/mL
形态 :powder
酸度系数(pKa) :7.50±0.20(Predicted)
颜色 :white to tan
InChIKey :MQIMZDXIAHJKQP-UHFFFAOYSA-N

安全信息

危险品标志 :Xn
危险类别码 :22-36
安全说明 :26
WGK Germany :3

普林贝瑞性质、用途与生产工艺

生物活性 Prinaberel (ERB-041) 是一种有效的选择性雌激素受体 β (ERβ) 激动剂，对人，大鼠和小鼠 ERβ 的 IC50 分别为 5.4、3.1 和 3.7 nM。 Prinaberel 对 ERβ 的选择性是 ERα 的 200 倍以上。Prinaberel是有效的皮肤癌化学预防剂，可通过抑制 WNT/β-catenin 信号通路发挥作用。Prinaberel 诱导卵巢癌细胞凋亡 (apoptosis)。

靶点

hERβ

5.4 nM (IC ₅₀ )

rat ERβ

3.1 nM (IC ₅₀ )

mouse ERβ

3.7 nM (IC ₅₀ )

hERα

1200 nM (IC ₅₀ )

mouse ERα

750 nM (IC ₅₀ )

rat ERα

620 nM (IC ₅₀ )

体外研究

Prinaberel (ERB-041) (0-60 µM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation.
Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and COX-2 in A431 cells. Prinaberel diminishes phosphorylated-PI3K and -AKT, which is associated with the enhancement in E-cadherin expression and reduction in migration of A431 cells.
Prinaberel (0.01-10 µM) inhibits cell proliferation in a dose- and time-dependent manner.
Prinaberel (10 µM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis.

Western Blot Analysis

Cell Line:	A431 cells
Concentration:	0, 20, 40 and 60 µM
Incubation Time:	24 hours
Result:	Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.

Cell Proliferation Assay

Cell Line:	SKOV-3, A2780CP or OVCAR-3 cells
Concentration:	0.01, 0.1 and 10 µM
Incubation Time:	24-48 hours
Result:	Showed significantly inhibitory effect on cell proliferation.

体内研究

Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice.
Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling.

Animal Model:	Six- to eight-weeks-old SKH-1 hairless female mice
Dosage:	2 mg/mouse in 200µl ethanol
Administration:	Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks
Result:	Diminished UVB-induced skin tumor development in SKH-1 hairless mice.