FB23-2
作者：齐岳
发布时间：2023-09-06
08:59:44
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产品名称：FB23-2
产品描述：
| 产品描述 | FB23-2 is a potent and selective mRNA N6-methyladenosine (m6A) demethylase FTO inhibitor(IC50 : 2.6 μM). |
| 靶点活性 | FTO:2.6 μM (IC50) |
| 体外活性 | FB23-2 directly bind to FTO and selectively inhibit FTO's m6A demethylase activity. Mimicking FTO depletion, FB23-2 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]. |
| 体内活性 | FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice[1]. |
| 细胞实验 | Quantitation of FB23 and FB23-2 in AML cells: NB4 and MONOMAC6 cells were treated with 10 μM FB23 or FB23-2 for 24 hr, respectively. Viable cells were distinguished with 0.1% trypan blue, counted and then harvested with PBS by several washings. Cells were diluted into 100 μl with 50% (v/v) water/methanol and followed by several shock freeze-thaw cycles. The supernatants were collected for analysis. The Ultimate 3000 system coupled with a TSQ Quantiva mass spectrometer was applied to determine the cellular concentration of compound FB23 and FB23-2. Analytes were separated on a XSELECT? HSS T3 column (100 mm × 3.0 mm, 2.5 μm). The mobile phases used for elution were (A) 0.1% (v/v) formic acid/water and (B) 0.1% (v/v) formic acid/acetonitrile. The mass spectrometer was operated in the negative MRM mode. Parent-to-product transitions were m/z 375.1→339.1, 375.1→298.1 for FB23, and m/z 390.3→318.0, 390.3→289.9 for FB23-2, respectively[1]. |
| 动物实验 | The NSGS mice were bred and subjected to the xeno-transplantation model. For the AML mouse model, 0.2 × 10^6 MONOMAC6 cells were directly transplanted into NSGS mice via tail vein. After 10 days, FB23-2 (2 mg/kg/day) and DMSO vehicle were intraperitoneally injected into the mice for a continuous 10 days. The mice were euthanized by CO2 inhalation if they exhibited classical AML symptoms including hunched posture, paralysis, and reduced body weight. Meanwhile, the PB, spleen, and liver samples were collected for further analysis[1]. |
| 分子量 | 392.24 |
| 分子式 | C18H15Cl2N3O3 |
| CAS No. | 2243736-45-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 62.5 mg/mL (159.34 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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