MX69

製品コードS8403 バッチS840301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₇H₂₆N₂O₄S

分子量

474.57

CAS No.

1005264-47-0

Solubility (25°C)*

体外

DMSO

95 mg/mL (200.18 mM)

Ethanol

41 mg/mL (86.39 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。	4.75mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 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。	0.675mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.5 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	MX69 is a MDM2/XIAP inhibitor, used for cancer treatment.
in vitro	MX69 inhibits expression of both MDM2 and XIAP in a time- and dose-dependent manner. This compound induces ubiquitination of endogenous MDM2 in cancer cells. Downregulation of MDM2 by this chemical is through induction of MDM2 self-ubiquitination and degradation. Half-life of MDM2 in control-treated EU-1 cells is greater than 90 min, whereas this compound treatment decreases the MDM2 half-life to <30 min. In SK-N-SH cells with stably transfected either wild-type (WT)-MDM2 or mutant MDM2-C464A, Treatment with this compound significantly inhibits expression and increased the turnover of WT-MDM2 but not MDM2-C464A. This compound significantly enhances the p53 half-life in WT-MDM2 but not mutant MDM2-C464A-transfected SK-N-SH cells. p53 is stabilized and accumulates in this compound-treated cells. This compound-mediated inhibition of XIAP is MDM2 dependent. Treatment of this chemical activates caspases 3, 7, and 9 as well as the cleavage of the death substrate PARP. This compound also exhibits a significant cytotoxic effect on both ALL and NB lines(cancer cell lines), particularly those lines with MDM2 overexpression and a WTp53 phenotype. This compound-induced cell death is indeed due to apoptosis. This compound-induced cell apoptosis and death are dependent on MDM2, p53, and XIAP expression. This compound shows minimal inhibitory effect on normal human bone marrow in vitro.
in vivo	MX69 has significant apoptotic and anti-proliferative effects on MDM2-expressing cancer cells in vivo. This compound is well tolerated in animals due to the fact that normal cells/tissues express little or no MDM2. No evidence of toxicity after treatment with this chemical at the 100 mg/kg dose. This MDM2-specific agent should not activate either on-target (e.g., p53 induction) or off-target signaling pathways in normal cells. Thus, specific MDM2 inhibitors such as this compound may be excellent candidates for targeted therapy of refractory cancers expressing high levels of MDM2.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	six ALL cell lines (EU-1, EU-3, EU-6, EU-8, SUP-B13, and UOC-B1) and six NB cell lines (NB-1691, NB-1643, SH-EP1, IMR-32, SK-NSH, and LA1-55N)
	濃度	0-10 μM
	反応時間	24 h
	実験の流れ	The cytotoxic effect of MX69 is determined using the WST assay. Briefly, cells cultured in 96-well microtiter plates are treated with different concentrations of this compound for a 20-hr period. WST (25 mg/well) is then added and incubation continued for an additional 4 hr, after which the optical density is read with a microplate reader.
動物実験	動物モデル	SCID mice
	投薬量	50, 75, and 100 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/27666947/

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：

CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer [ Cell Death Dis, 2024, 15(9):662]	PubMed: 39256356
High Glucose Treatment Limits Drosha Protein Expression and Alters AngiomiR Maturation in Microvascular Primary Endothelial Cells via an Mdm2-dependent Mechanism [ Cells, 2021, 10(4)742]	PubMed: 33801773

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。