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LY500307

Names

[ CAS No. ]:
533884-09-2

[ Name ]:
LY500307

[Synonym ]:
Erteberel
(3aS,4R,9bR)-4-(4-Hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
Benzo[b]cyclopenta[d]pyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aS,4R,9bR)-
(3aS,4R,9bR)-1,2,3,3a,4,9b-Hexahydro-4-(4-hydroxyphenyl)cyclopenta[c][1]benzopyran-8-ol
LY500307

Biological Activity

[Description]:

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Neurological Disease

[Target]

Ki: 1.54 nM (ERβ)[1] EC50: 3.61 nM[1]


[In Vitro]

Treatment with LY500307 significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro[2]. ERβ agonists promote apoptosis of GBM cells. It modulated several pathways related to apoptosis, cell cycle, and DNA damage response[2]. LY500307 sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide[2].

[In Vivo]

LY500307 treatment significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic model[2]. LY500307 treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model[2].

[References]

[1]. Zhao L, et al. Pharmacological activation of estrogen receptor beta augments innate immunity to suppress cancer metastasis. Proc Natl Acad Sci U S A. 2018 Apr 17;115(16):E3673-E3681.

[2]. Sareddy GR, et al. Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma. Sci Rep. 2016 Apr 29;6:24185.

Chemical & Physical Properties

[ Density]:
1.268

[ Boiling Point ]:
485.2±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H18O3

[ Molecular Weight ]:
282.33

[ Flash Point ]:
247.3±28.7 °C

[ Exact Mass ]:
282.125580

[ PSA ]:
49.69000

[ LogP ]:
3.84

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.639

Related Compounds