MI-463

製品コードS7816 バッチS781601

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

C₂₄H₂₃F₃N₆S

分子量

484.54

CAS No.

1628317-18-9

Solubility (25°C)*

体外

DMSO

96 mg/mL (198.12 mM)

Ethanol

22 mg/mL (45.4 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。	4.85mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 97 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。	0.68mg/ml (1.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.6 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	MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
in vitro	MI-463 demonstrates profound on-target activity in MLL leukemia cells. This compound results in substantial growth inhibition, with half-maximal growth inhibitory concentration (GI50) values of 0.23 μM, measured after 7 days of treatment in MLL leukemia cells. It is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of this chemical also leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of MLL fusion proteins substantially upregulated in MLL leukemias^[1].
in vivo	MI-463 shows substantial survival benefit in mouse models of MLL leukemia. It has very favorable druglike properties, including metabolic stability and PK profile in mice. This compound achieves high levels in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability(∼45%). In a mouse xenograft model using MV4;11 human MLL leukemia cells implanted into BALB/c nude mice, this chemical induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. It does not impair normal hematopoiesis in vivo^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	leukemia cells
	濃度	--
	反応時間	6 or 7 days
	実験の流れ	For viability assays, leukemia cells are plated at relevant concentrations and treated with compounds or 0.25% DMSO and cultured at 37°C for 7 days. Medium is changed at day 4, viable cell numbers are restored to the original concentration, and compounds are re-supplied. The MTT cell proliferation assay kit (Roche) is then used, and plates are read for absorbance at 570 nm using a PHERAstar BMG microplate reader. Effect of this compound on expression level is assessed by qRT-PCR after 6 days of incubation of compounds with cells, with medium changed and compound re-supply at day 3. For cell differentiation studies, leukemia cells are treated with this chemical for 7 days, then harvested, washed, and incubated with Pacific Blue rat anti-mouse CD11b antibody before being analyzed by flow cytometry.
動物実験	動物モデル	C57BL/6 mice
	投薬量	15 mg/kg
	投与方法	I.V.

参考

https://pubmed.ncbi.nlm.nih.gov/25817203/

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：

Targeting CDK9 inhibits the growth of KMT2A-rearranged infant leukemia and demonstrates synergy with menin inhibition [ Blood Neoplasia, 2025, 2(4):100148]	PubMed: 40979068
Therapeutic targeting of metabolic vulnerabilities in cancers with MLL3/4-COMPASS epigenetic regulator mutations [ J Clin Invest, 2023, 133(13)e169993]	PubMed: 37252797
The human leukemic oncogene MLL-AF4 promotes hyperplastic growth of hematopoietic tissues in Drosophila larvae [ iScience, 2023, 26(10):107726]	PubMed: 37720104
The human leukemic oncogene MLL-AF4 promotes hyperplastic growth of hematopoietic tissues in Drosophila larvae [ iScience, 2023, 26(10):107726]	PubMed: 37720104
Thioguanine Induces Apoptosis in Triple-Negative Breast Cancer by Regulating PI3K-AKT Pathway [ Front Oncol, 2020, 10:524922]	PubMed: 33194583

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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