849662-80-2
849662-80-2 structure
- Name: Y 134
- Chemical Name: [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]methanone
- CAS Number: 849662-80-2
- Molecular Formula: C28H28N2O3S
- Molecular Weight: 472.60
- Catalog: Research Areas Cancer
- Create Date: 2017-08-21 08:42:57
- Modify Date: 2024-02-26 10:24:43
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Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells[1].
| Name | [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]methanone |
|---|---|
| Synonyms |
hms3269l21
y 134 |
| Description | Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells[1]. |
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| Related Catalog | |
| Target |
ERα:0.09 nM (Ki) ERβ:11.31 nM (Ki) |
| In Vitro | Y134 exhibits potent antagonist activity at ERs in CV-1 cells cotransfected with plasmids containing ERα or ERβ and oestrogen-response element-driven luciferase, with IC50 [1]. Y134 (0.01 nM-10 μM; 6 d) inhibits the oestrogen-stimulated ER-expressing breast cancer cell (MCF-7 and T47D) proliferation[1]. Cell Viability Assay[1] Cell Line: MCF-7, T47, MDA-MB-231 cells Concentration: 0.01 nM-10 μM Incubation Time: 6 days Result: Suppressed oestrogen-stimulated MCF-7 and T47D cell proliferation. Showed no effects on MDA-MB-231 cells, except some cytotoxicity was seen at high concentrations. |
| In Vivo | Y134 (1-3 mg/kg/day; p.o. for 3 days) abolishes the E2-induced mammary gland terminal end bud (TEB) outgrowth in ovariectomized rats. Y134 inhibits uterine cell proliferation induced by E2 in a dose-dependent manner[1]. Animal Model: Four-week old female Sprague-Dawley rats were received ovariectomy[1] Dosage: 1, 3 mg/kg Administration: P.o. daily for 3 days Result: Abolished the effect exerted by E2 in a dose-dependent manner. |
| References |
| Density | 1.282g/cm3 |
|---|---|
| Boiling Point | 722.282ºC at 760 mmHg |
| Molecular Formula | C28H28N2O3S |
| Molecular Weight | 472.60 |
| Flash Point | 390.623ºC |
| Exact Mass | 472.18200 |
| PSA | 92.25000 |
| LogP | 5.74380 |
| Index of Refraction | 1.673 |