Imlunestrant
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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.96%
- No. CAS: 2408840-26-4
- Fòrmula: C29H24F4N2O3
- Peso molecular:524.51
-
Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
Drug Repurposing Compound Library
HY-L035
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Breast Cancer Compound Library
HY-L074
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Nuclear Receptor Compound Library
HY-L126
-
Heterocyclic Compound Library
HY-L138
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) Imlunestrant
More
Actividad biológica
|
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] |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 2408840-26-4
-
Appearance Solid
-
Peso molecular 524.51
-
Fòrmula 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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (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)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| 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 |
Powered by Bioz