Prinaberel

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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)。

Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.

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.

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 weeksResult:Diminished UVB-induced skin tumor development in SKH-1 hairless mice.

——

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen/progestogen Receptor

——

——

524684-52-4

271.24

C15H10FNO3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 40 mg/mL (147.47 mM)

Oc1cc(C=C)c2oc(nc2c1)-c1ccc(O)c(F)c1

——

(-20℃)

With Ice Pack

≥ 2 years