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Imlunestrant Estrogen/progestogen Receptor Antagonist

Name: Imlunestrant
Brand: Selleck Chemicals
SKU: E1301
Rating: 5 (1 reviews)

Cat.No.: E1301

Imlunestrant(LY3484356) is a potent, orally bioavailable selective oestrogen receptor degrader (SERD) that functions as a pure antagonist of oestrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of oestrogen-driven growth in ER-positive cells.

Chemical Structure

Molecular Weight: 524.51

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Quality Control

Batch: E130101 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 96.07%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

96.07

Related Targets	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES
Other Estrogen/progestogen Receptor Inhibitors	Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Kaempferol Cholesterol PHTPP G15 Licochalcone A Endoxifen HCl Pregnenolone

Chemical Information, Storage & Stability

Molecular Weight	524.51	Formula	C₂₉H₂₄F₄N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2408840-26-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (190.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	ER-α
References	[1] https://pubmed.ncbi.nlm.nih.gov/34360578/ [2] https://ascopubs.org/doi/abs/10.1200/JCO.2021.39.15_suppl.1050

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-07)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05768139	RECRUITING	Breast Cancer; Solid Tumors, Adult	Eli Lilly and Company	2023-04-17	PHASE1; PHASE2
NCT07191717	RECRUITING	Anatomic Stage I Breast Cancer AJCC v8; Anatomic Stage II Breast Cancer AJCC v8; Anatomic Stage III Breast Cancer AJCC v8; Invasive Breast Carcinoma; Localized Estrogen Receptor-Positive Breast Carcinoma; Localized Human Epidermal Growth Factor Receptor (HER2)-Negative Breast Carcinoma	Jonsson Comprehensive Cancer Center	2026-05-18	PHASE2
NCT07410559	NOT_YET_RECRUITING	Breast Cancer	Fudan University	2026-07-01	PHASE2
NCT07287098	RECRUITING	Breast Neoplasms	Eli Lilly and Company	2026-05-13	PHASE2
NCT05514054	ACTIVE_NOT_RECRUITING	Breast Neoplasms	Eli Lilly and Company	2022-10-04	PHASE3
NCT05307705	RECRUITING	Breast Cancer	Eli Lilly and Company	2022-05-11	PHASE1

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