H3B-5942

製品コードS8746 バッチS874601

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₃₁H₃₄N₄O₂

分子量

494.63

CAS No.

2052128-15-9

Solubility (25°C)*

体外

DMSO

99 mg/mL (200.14 mM)

Ethanol

13 mg/mL (26.28 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5mg/ml (10.11mM)	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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.71mg/ml (1.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.
in vitro	H3B-5942 covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation. Upon binding to ERα, this compound triggers global DNA binding of ERα to ERE-containing promoter and enhancer regions and induces a transcriptionally repressive conformation of ERα by evicting coactivators. It demonstrates potent antiproliferative activity in a panel of ERα^WT and ERα^MUT lines with GI50 values of 0.5, 2, and 30 nmol/L in the MCF7-Parental, MCF7-LTED-ERα^WT, and MCF7-LTED-ERα^Y537C lines, respectively. In the absence of E2, this chemical shows no significant impact on ER-mediated transcription in the MCF7-Parental (endocrine therapy-sensitive) and MCF7-LTED-ERαY537C lines but does result in a 1.5-fold (P = 0.03) increase in the MCF7-LTED-ERα^WT line. In the presence of E2, it shows a significant dose-dependent decrease in ER-mediated transactivation in all cell lines tested^[1].
in vivo	In vivo, H3B-5942 demonstrates significant single-agent antitumor activity in xenograft models representing ERαWT and ERαY537S breast cancer^[1].

プロトコル(参考用のみ)

動物実験	動物モデル	Mice bearing PDX tumors representing Erα(Y537S/WT) breast cancer
	投薬量	3, 10, 30, 100, and 200 mg/kg
	投与方法	PO

参考

https://pubmed.ncbi.nlm.nih.gov/29991605/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Ginsenoside Rd Activates Ciliary Beat Frequency via Estrogen Receptor β and P2X7 Receptor [ Biol Pharm Bull, 2025, 48(5):657-671]	PubMed: 40399102
SPACe: an open-source, single-cell analysis of Cell Painting data [ Nat Commun, 2024, 15(1):10170]	PubMed: 39580445
Novel Estrogen Receptor Dimerization BRET-Based Biosensors for Screening Estrogenic Endocrine-Disrupting Chemicals [ Biomater Res, 2024, 28:0010]	PubMed: 38464469

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。