FB23-2

製品コードS8837 バッチS883702

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式

C18H15Cl2N3O3

分子量 392.24 CAS No. 2243736-45-8
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 78 mg/mL (198.85 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)
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 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。

1.250mg/ml (3.19mM) Taking the 1 mL working solution as an example, add 50 μL of 25 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 40%PEG300 5%Tween80 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。

0.550mg/ml (1.40mM) Taking the 1 mL working solution as an example, add 50 μL of 11 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 FB23-2 is a potent and selective FTO inhibitor that directly binds to FTO and selectively inhibits FTO's N6-methyladenosine (m6A) demethylase activity with IC50 of 2.6 μM.
in vitro

FB23-2 directly binds to FTO and selectively inhibits its m6A demethylase activity. Mimicking FTO depletion, this compound dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro.[1]

in vivo

FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Leukemia cells NB4, U937, MV4-11, ML-2; MONOMAC6 (ACC-124) cells; 293T cells; The mouse bone marrow cells FLT3ITD/NPM1, MA9
濃度 10 μM, 5 μM
反応時間 24 h, 72 h
実験の流れ

NB4 and MONOMAC6 cells are treated with DMSO or FB23-2 at varying concentrations for 72 h, while MA9 and FLT3/NPM1 primary cells isolated from AML mice, five human AML cell (MA9.3ITD, MA9.3RAS, U937, ML2, and MV4-11), and human primary AML cells are treated with DMSO or 5 μM of this compound for 72 h for dot blot assay.

動物実験 動物モデル NSGS mice with xeno-transplantation model
投薬量 2 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/30991027/

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:

FTO suppresses DNA repair by inhibiting PARP1 [ Nat Commun, 2025, 16(1):2925] PubMed: 40133293
Hypoxia-induced degradation of FTO promotes apoptosis by unmasking RACK1-mediated activation of MTK1-JNK1/2 pathway [ J Adv Res, 2025, S2090-1232(25)00038-4] PubMed: 39805423
RNA N6-methyladenosine demethylase FTO promotes diabetic wound healing through TRIB3-mediated autophagy in an m6A-YTHDF2-dependent manner [ Cell Death Dis, 2025, 16(1):222] PubMed: 40157922
NRF2 maintains redox balance via ME1 and NRF2 inhibitor synergizes with venetoclax in NPM1-mutated acute myeloid leukemia [ Cancer Metab, 2025, 13(1):32] PubMed: 40533864
YTHDF2 upregulation and subcellular localization dictate CD8 T cell polyfunctionality in anti-tumor immunity [ Nat Commun, 2024, 15(1):9559] PubMed: 39500904
m6A eraser FTO impairs gemcitabine resistance in pancreatic cancer through influencing NEDD4 mRNA stability by regulating the PTEN/PI3K/AKT pathway [ J Exp Clin Cancer Res, 2023, 42(1):217] PubMed: 37605223
Targeting AKT induced Ferroptosis through FTO/YTHDF2-dependent GPX4 m6A methylation up-regulating and degradating in colorectal cancer [ Cell Death Discov, 2023, 9(1):457] PubMed: 38102129
Cytoplasmic Expression of TP53INP2 Modulated by Demethylase FTO and Mutant NPM1 Promotes Autophagy in Leukemia Cells [ Int J Mol Sci, 2023, 24(2)1624] PubMed: 36675134
m6A demethylase FTO renders radioresistance of nasopharyngeal carcinoma via promoting OTUB1-mediated anti-ferroptosis [ Transl Oncol, 2023, 27:101576] PubMed: 36343416
E6E7 regulates the HK2 expression in cervical cancer via GSK3β/FTO signal [ Arch Biochem Biophys, 2022, 729:109389] PubMed: 36075458

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。