Mezigdomide (CC-92480)

製品コードS8975 バッチS897502

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₃₂H₃₀FN₅O₄

分子量

567.61

CAS No.

2259648-80-9

Solubility (25°C)*

体外

DMSO

100 mg/mL (176.17 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% corn oil	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. 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	Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
in vitro	CC-92480 has a unique and rapid degradation profile: the enhanced efficiency to drive the formation of the protein−protein interaction between Aiolos and cereblon, inducing targeted docking to the CRL4-CRBN E3 ubiquitin ligase complex. The CC-92480-dependent binding of Aiolos/Ikaros to CRBN leads to polyubiquitination and ultimately proteasome-mediated degradation of protein. Rapid and extensive loss of Aiolos/Ikaros in sensitive cells, such as multiple myeloma cells, results in apoptosis and subsequent cell death.^[1]
in vivo	CC-92480 is evaluated in efficacy models to assess tumor growth inhibition in tumor bearing mice. When tumors reaches approximately 150 mm³, mice are randomized and treated once daily (q.d.) orally with vehicle control or various dosage strengths of CC-92480. Both the 3 and 10 mg/kg doses give near maximal response in this model, while the lowest dose tested (1 mg/kg) shows 75% reduction in tumor volume by the end of the study.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	H929 R10-1 cells
	濃度	1 nM, 10 nM, 100 nM
	反応時間	4 h, 72 h
	実験の流れ	H929 R10-1 cells are treated with DMSO and CC-92480 for 4 h and 72 h. Cells are then washed with 1× PBS and lysed in Chris buffer.
動物実験	動物モデル	Female 6−8 weeks old CB17 SCID mice; Sprague-Dawley rats
	投薬量	1 mg/kg, 3 mg/kg, 10 mg/kg; 2 mg/kg
	投与方法	Oral gavage; IV

参考

[1] Joshua D Hansen, et al. J Med Chem. 2020 Jul 9;63(13):6648-6676.

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：

IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666]	PubMed: 36822576
IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666]	PubMed: 36822576

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。