MI-136

製品コードS7815 バッチS781501

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

C₂₃H₂₁F₃N₆S

分子量

470.51

CAS No.

1628316-74-4

Solubility (25°C)*

体外

DMSO

94 mg/mL (199.78 mM)

Ethanol

94 mg/mL (199.78 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.

* <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-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.
in vitro	MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to this compound. Treatment with this chemical also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with this compound induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage and blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of this inhibitor on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer^[1].
in vivo	Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	VCaP cells
	濃度	5 μM
	反応時間	48 h
	実験の流れ	To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM of this compound for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and this chemical for 48 hrs. Cells are then stimulated with 10nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays.
動物実験	動物モデル	VCaP tumor-bearing mice（VCaP xenografts）
	投薬量	40 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/25822367/

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：

Combinatorial targeting of a chromatin complex comprising Dot1L, menin and the tyrosine kinase BAZ1B reveals a new therapeutic vulnerability of endocrine therapy-resistant breast cancer [ Breast Cancer Res, 2022, 24(1):52]	PubMed: 35850772
Combinatorial targeting of menin and the histone methyltransferase DOT1L as a novel therapeutic strategy for treatment of chemotherapy-resistant ovarian cancer [ Cancer Cell Int, 2022, 22(1):336]	PubMed: 36333801
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model [ J Med Chem, 2020, 31]	PubMed: 32191458

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。