FB23-2
作者：齊岳
發(fā)布時間：2023-09-06
08:59:44
點擊數(shù)：
產(chǎn)品名稱：FB23-2
產(chǎn)品描述：
| 產(chǎn)品描述 | FB23-2 is a potent and selective mRNA N6-methyladenosine (m6A) demethylase FTO inhibitor(IC50 : 2.6 μM). |
| 靶點活性 | FTO:2.6 μM (IC50) |
| 體外活性 | 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]. |
| 體內(nèi)活性 | FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice[1]. |
| 細胞實驗 | 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]. |
| 動物實驗 | 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 |
存儲
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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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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