2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Imlunestrant

Imlunestrant  (Synonyms: LY-3484356)

製品番号: HY-145572 純度: 99.96% ee.: 100.00%
COA 取扱説明書 Technical Support

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).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Imlunestrant

Imlunestrant 構造式

CAS 番号 : 2408840-26-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 225 在庫あり
Solution
10 mM * 1 mL in DMSO USD 225 在庫あり
Solid
5 mg $195 在庫あり
10 mg $305 在庫あり
25 mg $495 在庫あり
50 mg $690 在庫あり
100 mg $970 在庫あり
250 mg $1460 在庫あり
500 mg $2100 在庫あり
1 g $2950 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Imlunestrant:

Imlunestrant 関連抗体

Top Publications Citing Use of Products

Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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)[1][2].

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
3 1
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]
MCF7 IC50
17 1
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
17 1
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 1
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]
体外実験

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.

Imlunestrant 関連抗体
臨床実験
分子量

524.51

分子式

C29H24F4N2O3
CAS 番号
Appearance

Solid

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.96% ee.: 100.00%

COA (247 KB) HNMR (532 KB) CNMR (653 KB) RP-HPLC (263 KB) NP-HPLC (244 KB) LCMS (93 KB)

取扱説明書 (2659 KB)
参考文献

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
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Imlunestrant Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Imlunestrant2408840-26-4LY-3484356LY3484356LY 3484356Estrogen Receptor/ERRSERDER+HER2breast cancerInhibitorinhibitorinhibit

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製品名:
Imlunestrant
製品番号:
HY-145572
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