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FB23-2

FB23-2

产品编号 T7138   CAS 2243736-45-8

FB23-2 是一种 mRNA N6- 甲基腺嘌呤脱甲基酶 FTO 选择性抑制剂,IC50值为 2.6 μM。它具有抗增殖作用,可研究急性髓系白血病。

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FB23-2 Chemical Structure
FB23-2, CAS 2243736-45-8
规格 价格/CNY 货期 数量
1 mg ¥ 397 现货
2 mg ¥ 582 现货
5 mg ¥ 898 现货
10 mg ¥ 1,630 现货
25 mg ¥ 2,780 现货
50 mg ¥ 4,130 现货
100 mg ¥ 5,890 现货
500 mg ¥ 11,900 现货
1 mL * 10 mM (in DMSO) ¥ 997 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: FB23-2 (T7138)
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纯度: 98.91%
纯度: 98%
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参考文献
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直接与FTO结合,选择性抑制FTO的m6A去甲基化酶活性。模拟FTO耗尽,FB23-2显著抑制人急性髓性白血病(AML)细胞系和原代AML细胞的增殖,并促进其分化/凋亡 in vitro[1]。
体内活性 FB23-2在异种移植小鼠中显著抑制人类AML细胞系和原代细胞的进展[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 1 year

溶解度

DMSO: 62.5 mg/mL (159.34 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5495 mL 12.7473 mL 25.4946 mL 63.7365 mL
5 mM 0.5099 mL 2.5495 mL 5.0989 mL 12.7473 mL
10 mM 0.2549 mL 1.2747 mL 2.5495 mL 6.3736 mL
20 mM 0.1275 mL 0.6374 mL 1.2747 mL 3.1868 mL
50 mM 0.051 mL 0.2549 mL 0.5099 mL 1.2747 mL
100 mM 0.0255 mL 0.1275 mL 0.2549 mL 0.6374 mL

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TargetMol Library Books参考文献

1. Huang Y , Su R , Sheng Y , et al. Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia[J]. Cancer Cell, 2019, 35(4):677-691.e10. 2. Inge V D W , Jamieson C . The Yin and Yang of RNA Methylation: An Imbalance of Erasers Enhances Sensitivity to FTO Demethylase Small-Molecule Targeting in Leukemia Stem Cells[J]. Cancer Cell, 2019, 35(4):540-541.
Goserelin acetate Bullatine A Chelidonine GSK2656157 BG45 Chelerythrine chloride CCT018159 Zoledronic Acid

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 已知活性化合物库 血液病分子库 细胞凋亡化合物库 NO PAINS 化合物库 抗肥胖化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

FB23-2 2243736-45-8 Apoptosis Others FB23 2 AML leukemia acute anti-proliferation Inhibitor FB232 m6A myeloid mRNA inhibit demethylase FB-23-2 inhibitor

 

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