Fig. 1 · Structure

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Erteberel (LY500307)

Cat. No. A10550 CAS 533884-09-2

ERβ agonist

LY500307 is a potent, selective estrogen receptor beta agonist with an EC50 of 0.66 nM.

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Biological Activity

Target & Activity

Target Activity Value
ERβ Ki 1.54 nM
ERβ EC50 3.61 nM

Cellular Effect

Cell Line Activity Value Description Reference
PC-3 EC50 0.66 nM Activity at ERbeta in PC3 cells by transcription assay [PMID: 17034120]
PC-3 EC50 19.4 nM Activity at ERalpha in PC3 cells by transcription assay [PMID: 17034120]

In Vitro Studies

Erteberel (LY500307) treatment altered gene expression in SKOV3-ALDH+ OCSCs compared with vehicle, with 596 differentially expressed genes. In a study using MyLa cells, treatment significantly reduced viability across 4 different CTCL cell lines in a dose-dependent manner. In U87 GBM cells, treatment yielded 3204 differentially expressed genes. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Gene expression changes in SKOV3-ALDH+ OCSCs

Cell-based study · SKOV3-ALDH+ OCSCs [1]

SKOV3-ALDH+ OCSCs were treated with Erteberel (LY500307) at 5 µM for 24 h. Compared with vehicle, treatment identified 596 differentially expressed genes, including 382 upregulated genes and 214 downregulated genes.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
differentially expressed genes (DEGs)differentially expressed genes 596 genes[1]

Literature-Reported Treatment Conditions

Treatment concentration
5 µM
Exposure duration
24 h
Co-treatment
Other interventions in this design: B27 serum free supplement; EGF 20 ng/mL; bFGF 20 ng/mL; hydrocortisone 0.5 μg/mL; insulin 5 μg/mL. Compound effect isolated by the comparison: Compared with vehicle.
Reported limits
Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Erteberel (LY500307); Compound label in the paper: LY-500307

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

2. Results > 2.3. Analysis of Transcriptional Changes Altered by LY500307 Treatment in OCSCs (S31); 4. Materials and Methods > 4.2. Isolation of OCSCs and Cell Viability Assays (S75); 4. Materials and Methods > 4.6. RNA-Sequencing (S106, S108)

differentially expressed genes (DEGs): differentially expressed genes (DEGs); comparator: vehicle — 2. Results > 2.3. Analysis of Transcriptional Changes Altered by LY500307 Treatment in OCSCs (S31); 4. Materials and Methods > 4.6. RNA-Sequencing (S108)

Reduced viability in CTCL cell lines

Cell-based study · MyLa [2]

MyLa cells were treated with varying concentrations of Erteberel (LY500307) for 48 hours, with viability assessed using MTS assays. The reported result was significantly reduced viability in 4 different CTCL cell lines in a dose-dependent manner.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
MTS cell viability assaysReported result Treatment with LY500307 significantly reduced the viability in 4 different CTCL cell lines in a dose-dependent manner[2]

Literature-Reported Treatment Conditions

Treatment concentration
varying concentrations
Exposure duration
48 hours
Vehicle
dimethyl sulfoxide
Reported limits
Not stated in the sentences used: route.
Methods and source locations

Compound reported in the paper: Erteberel (LY500307); Compound label in the paper: LY-500307

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Cell culture and reagents (S2); Methods > Cell viability (S20, S21); Results > Selective ERβ agonist LY500307 enhances ERβ signaling and reduces cell viability in CTCL cells (S90, S91); Figure 1. legend (S138, S140)

MTS cell viability assays: MTS cell viability assays; comparator: cells treated with dimethyl sulfoxide (DMSO; untreated Ctrl) — Results > Selective ERβ agonist LY500307 enhances ERβ signaling and reduces cell viability in CTCL cells (S90, S91)

Gene expression changes in GBM cells

Cell-based study · U87 GBM cells [3]

U87 GBM cells were treated with Erteberel (LY500307) at 5 μM for 48 h. RNA-seq analysis identified 3204 differentially expressed genes, including 1568 upregulated genes and 1636 downregulated genes.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
RNA-seq analysisdifferential gene expression 3204 genes[3]

Literature-Reported Treatment Conditions

Treatment concentration
5 μM
Exposure duration
48 h
Reported limits
Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Erteberel (LY500307); Compound label in the paper: LY-500307

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Analysis of LY500307 induced global transcriptional changes in GBM cells (S27, S29); Materials and Methods > RNA sequencing and qRT-PCR (S119)

RNA-seq analysis: RNA-seq analysis; comparator: vehicle — Results > Analysis of LY500307 induced global transcriptional changes in GBM cells (S27, S29)

In Vivo Studies

Erteberel (LY500307) was administered by oral gavage to nude mice bearing intracranially implanted U251 GBM-luc cells at 5 mg/kg body weight/day for 28 days. Compared with vehicle, treatment inhibited GBM progression, assessed by luciferase intensity. [3]

GBM progression in nude mice

Animal study · U251 GBM-luc cells were implanted intracranially into the right striatum of nude mice; n = 5 [3]

Nude mice bearing intracranially implanted U251 GBM-luc cells received Erteberel (LY500307) by oral gavage at 5 mg/kg body weight/day for 28 days. Compared with vehicle, treatment inhibited GBM progression, assessed by luciferase intensity.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor growth in terms of luciferase intensityReported result LY500307 inhibits the GBM progression in vivo[3]

Conditions shared by the study groups

Route
oral gavage
Treatment course
28 days
Vehicle
30% captisol
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Erteberel (LY500307) 5 mg/kg body weight/dayvehicleLY500307 inhibits the GBM progression in vivo[3]
Erteberel (LY500307) 5 mg/kg body weight/day
Model: U251 GBM-luc cells were implanted intracranially into the right striatum of nude mice; n = 5
Methods and source locations

Compound reported in the paper: Erteberel (LY500307); Compound label in the paper: LY-500307

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > LY500307 reduces GBM progression in an orthotopic model (S50, S52, S56); Materials and Methods > Cell viability and colony formation assays (S84, S90); Materials and Methods > Annexin V apoptosis assay (S95); Materials and Methods > In Vivo Orthotopic Tumor Models (S160, S163); Figure 6 legend (S199, S200, S201)

Tumor growth in terms of luciferase intensity: Tumor growth in terms of luciferase intensity; comparator: vehicle — Results > LY500307 reduces GBM progression in an orthotopic model (S56); Figure 6 legend (S201)

Erteberel (LY500307) 5 mg/kg body weight/day · Results > LY500307 reduces GBM progression in an orthotopic model (S50, S56); Figure 6 legend (S200)

Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 533884-09-2
Applications ERβ agonist
Formula C18H18O3
Molecular Weight 282.3
Synonyms Erteberel
SMILES
C1C[C@H]2[C@@H](C1)C3=C(C=CC(=C3)O)O[C@H]2C4=CC=C(C=C4)O

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] He Y, Alejo S, Venkata PP, et al. Therapeutic Targeting of Ovarian Cancer Stem Cells Using Estrogen Receptor Beta Agonist. Int J Mol Sci (2022). PMID: 35806169 DOI: 10.3390/ijms23137159 Source material
  2. [2] Özistanbullu D, Wilhelm R, Reichenbach G, et al. Estrogen receptor β stimulation as a possible novel therapeutic target for cutaneous T-cell lymphoma. Blood Adv (2025). PMID: 40020159 DOI: 10.1182/bloodadvances.2024015132 Source material
  3. [3] Sareddy GR, Li X, Liu J, et al. Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma. Sci Rep (2016). PMID: 27126081 DOI: 10.1038/srep24185 Source material

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