Art. -Nr.: HY-145572

Imlunestrant

(Synonyms: LY-3484356)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).

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Reinheit: 99.96%
CAS. Nr.: 2408840-26-4
Formel: C₂₉H₂₄F₄N₂O₃
Molecular Weight:524.51

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Imlunestrant Chemical Structure

CAS. Nr.: 2408840-26-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	17 nM Compound: 16; LY3484356	Antiproliferative activity against human MCF7 cells harboring ERalpha Y537N mutant assessed as inhibition of cell growth incubated for 6 to 7 days by high content imaging assay Antiproliferative activity against human MCF7 cells harboring ERalpha Y537N mutant assessed as inhibition of cell growth incubated for 6 to 7 days by high content imaging assay	[PMID: 37377342]
MCF7	IC₅₀	3 nM Compound: 16; LY3484356	Antiproliferative activity against human MCF7 cells harboring wild type ERalpha assessed as inhibition of cell growth incubated for 6 to 7 days by high content imaging assay Antiproliferative activity against human MCF7 cells harboring wild type ERalpha assessed as inhibition of cell growth incubated for 6 to 7 days by high content imaging assay	[PMID: 37377342]

In Vitro

LY3484356 shows favorable pharmacokinetic (PK) properties, including antitumor activity in ESR1 mutants^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2408840-26-4
Appearance Solid
Molecular Weight 524.51
Formel C₂₉H₂₄F₄N₂O₃
Color Light yellow to yellow
SMILES

OC1=CC2=NC=C(C3=CC=C(C(F)(F)F)C=C3O[C@]4([H])C5=CC=C(C=C5)OCCN6CC(C6)CF)C4=C2C=C1
Synonyms

LY-3484356
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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JCI Insight

Imlunestrant a next-generation oral SERD overcomes ESR1 mutant resistance in estrogen receptor-positive breast cancer. [Abstract]

2025 May 6:e188051. PMID: 40327396

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (190.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9065 mL

9.5327 mL

19.0654 mL

5 mM

0.3813 mL

1.9065 mL

3.8131 mL

10 mM

0.1907 mL

0.9533 mL

1.9065 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Komal L. Jhaveri, et al. A first-in-human phase 1a/b trial of LY3484356, an oral selective estrogen receptor (ER) degrader (SERD) in ER+ advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC): Results from the EMBER study. 2021 ASCO Annual Meeting I.

[2]. Cristina Hernando, et al. Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective. Int. J. Mol. Sci. 2021, 22(15), 7812.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9065 mL	9.5327 mL	19.0654 mL	47.6635 mL
	5 mM	0.3813 mL	1.9065 mL	3.8131 mL	9.5327 mL
	10 mM	0.1907 mL	0.9533 mL	1.9065 mL	4.7664 mL
	15 mM	0.1271 mL	0.6355 mL	1.2710 mL	3.1776 mL
	20 mM	0.0953 mL	0.4766 mL	0.9533 mL	2.3832 mL
	25 mM	0.0763 mL	0.3813 mL	0.7626 mL	1.9065 mL
	30 mM	0.0636 mL	0.3178 mL	0.6355 mL	1.5888 mL
	40 mM	0.0477 mL	0.2383 mL	0.4766 mL	1.1916 mL
	50 mM	0.0381 mL	0.1907 mL	0.3813 mL	0.9533 mL
	60 mM	0.0318 mL	0.1589 mL	0.3178 mL	0.7944 mL
	80 mM	0.0238 mL	0.1192 mL	0.2383 mL	0.5958 mL
	100 mM	0.0191 mL	0.0953 mL	0.1907 mL	0.4766 mL

Keywords

Imlunestrant

1 Cited Publications

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Imlunestrant

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Publications Citing Use of MedChemExpress (MCE) Imlunestrant

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Imlunestrant

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Breast Cancer Compound Library

FDA-Approved Anticancer Drug Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Imlunestrant

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Imlunestrant Related Classifications

HY-145572 Related Classifications