LY500307

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

LY500307 (LY-500307, Erteberel, SERBA-1) 是一种有效的选择性雌激素受体 β (ERβ) 激动剂，Ki/EC50 为 0.19/0.66 nM。

LY500307 (LY-500307, Erteberel, SERBA-1) is a potent, selective Estrogen Receptor β (ERβ) agonist with Ki/EC50 of 0.19/0.66 nM, 12-fold higher affinity than ERα and exhibits 32-fold more functional potency; reduces proliferation and induces apoptosis in GBM cells, enhances ERβ signaling and expression, modulates the expression of genes involved in cell cycle, cell death, survival, and DNA damage response; also sensitizes GBM cells to chemotherapeutic agents, reduces GBM progression in an orthotopic model .Schizophrenia Phase 2 Clinical.

Treatment with Erteberel (0.25-10 μM, 72 hours) significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro. Erteberel promotes apoptosis of GBM cells. Erteberel modulated several pathways related to apoptosis, cell cycle, and DNA damage response. Erteberel (0-1000 μM) sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide.Cell Viability Assay Cell Line:U87, U251,T98G and normal astrocytesConcentration:0.25, 0.5, 1, 2, 4, 6, 8, and 10 μMIncubation Time:72 h Result:Treatment with Erteberel significantly reduces the viability of various GBM cell lines in a dose-dependent manner. In contrast, viability of normal astrocytes is not affected at the tested doses, suggesting that Erteberel has tumor cell–specific activity.

Erteberel (5?mg/Kg body weight/day, oral, 28 days) treatment significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic model.Erteberel (5?mg/Kg body weight/day, oral, 40-50 days) treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model. Animal Model:Athymic mice (5-7 weeks) inoculated with OVCAR-3 cells Dosage:5mg/Kg body weight Administration:Oral, daily for 28 days Result:Immunohistochemical analysis reveals that Erteberel treatment significantly reduces the number of proliferation marker Ki-67-positive cells and increases the number of TUNEL-positive apoptotic cells.

LY-500307 | LY 500307 | Erteberel | SERBA-1

Endocrinology/Hormones

Estrogen Receptor/ERR

ERβ

Neurological Disease

Schizophrenia

533884-09-2

282.339

C18H18O3

>98% (HPLC)

In Vitro:?DMSO : ≥ 30 mg/mL (106.26 mM)

OC1=CC=C2C([C@@](CCC3)([H])[C@@]3([H])[C@H](C4=CC=C(O)C=C4)O2)=C1

(3aS,4R,9bR)-1,2,3,3a,4,9b-Hexahydro-4-(4-hydroxyphenyl)cyclopenta[c][1]benzopyran-8-ol

(-20℃)

With Ice Pack

≥ 2 years