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FB 23
冻存
10mg/支
FB23 Chemical Structure
CAS No. : 2243736-35-6
FB23 是一种有效的，选择性的 FTO 去甲基化酶抑制剂，IC50 为 60 nM。FB23 直接与 FTO 结合并选择性抑制 FTO 的 mRNA N6-甲基腺嘌呤脱甲基酶活性。
| 规格 | 10 mg/支 |
| 货号 | Gab-2022132 |
| 生物活性 | FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity[1]. |
| IC50 & Target | IC50: 60 nM (FTO)[1] |
| 体外研究 (In Vitro) |
FB23 (72 hours) treatment inhibits acute myeloid leukemia (AML) cells proliferation with IC50 values of 44.8 μM, 23.6 μM for NB4 and MONOMAC6 AML cells[1]. |
| FB23 treatment causes the significant suppression of MYC targets, E2F targets, and G2M checkpoint signal cascades, which may contribute to the inhibitory effects of FTO inhibitors and FTO KD on cell cycle and proliferation. FB23 treatments activates apoptosis and p53 pathways[1]. | |
| We has not independently confirmed the accuracy of these methods. They are for reference only. | |
| 体内研究 (In Vitro) |
A single dose of 3 mg/kg FB23 is i.p. administrated to Sprague Dawley (SD) rats for the pharmacokinetic profile. The Cmax and Tmax value of FB23 are 142.5 ng/mL and 0.4 hr, respectively[1]. |
| We has not independently confirmed the accuracy of these methods. They are for reference only. | |
| 分子量 | 377.22 |
| Formula | C₁₈H₁₄Cl₂N₂O₃ |
| CAS 号 | 2243736-35-6 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Powder -20°C 3 years |
| 4°C 2 years | |
| In solvent -80°C 6 months | |
| -20°C 1 month |
参考文献
| [1]. Yue Huang, et al. Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia. Cancer Cell. 2019 Apr 15;35(4):677-691.e10. |
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