MS1943

製品コードS8918 バッチS891803

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₄₂H₅₄N₈O₃

分子量

718.93

CAS No.

2225938-17-8

Solubility (25°C)*

体外

DMSO

100 mg/mL (139.09 mM)

Ethanol

50 mg/mL (69.54 mM)

Water

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	5.0mg/ml	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.

* <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	MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.

生物活性

製品説明	MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.
in vitro	MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells. MS1943 mediates its cytotoxic effects through ER stress and UPR induction in cells that are dependent for their growth on EZH2.^[1]
in vivo	MS1943 is efficacious in vivo and well tolerated in mice at the efficacious dose, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-MB-468 cells, HCC70 cells, BT549, HCC70 and MDA-MB-231 TNBC cells, KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells
	濃度	5 μM, 4 μM
	反応時間	24 h, 6 h
	実験の流れ	For the study using MDA-MB-468 cells, cells are cultured for 24 h in the presence of MS1943 (5 μM), alone or with different concentrations of the proteasome inhibitor MG132, and EZH2 protein levels are detected via western blot as described already. Vinculin is used as a loading control to normalize EZH2 protein levels. For the study using HCC70 cells, cells are cultured for 6 h in the presence of MS1943 (4 μM), alone or with different concentrations of MG132, and EZH2 protein levels are detected via western blot as described before. Actin is used as a loading control to normalize EZH2 protein levels.
動物実験	動物モデル	eight-week-old female BALB/c nude mice
	投薬量	150 mg/kg
	投与方法	IP

参考

[1] Anqi Ma, et al. Nat Chem Biol. 2020 Feb;16(2):214-222.

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。

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