FB23-2

目录号: GC36032纯度: >99.50%

FB23-2是一种mRNA N6-甲基腺嘌呤(M6A)脱甲基酶FTO的选择性抑制剂(IC50 = 2.6μM),可用于急性髓系白血病(AML)的研究。


FB23-2
Cas No.: 2243736-45-8
规格价格库存数量操作
1mg¥336.00现货
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5mg¥840.00现货
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10mg¥1,435.00现货
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50mg¥3,150.00现货
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10mM (in 1mL DMSO)¥924.00现货
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产品描述 Description

FB23-2 is a selective inhibitor of mRNA N6-methyladenine (M6A) demethylase FTO (IC50 = 2.6μM)[1]. It is can be used in research related to acute myeloid leukemia (AML)[1].

FB23-2 (72 hours) inhibited the proliferation of NB4 and MONOMAC6 cells, with an IC50 of 0.8μM and 1.5μM. FB23-2 (10μM, 96 hours) can significantly enhance the sensitivity of nasopharyngeal carcinoma (NPC) cells to irradiation[2].

FB23-2 (2mg/kg/d, 10 days, i.p.) significantly inhibited the progression of acute myeloid leukemia (AML) and extended survival in AML mice[1]. FB23-2 (8mg/kg/d, 14 days, i.p.) significantly inhibited tumor growth and prolonged survival time in clear cell renal cell carcinoma (ccRCC) mouse model[3]. FB23–2 (2mg/kg/day, 3 days, intrabitoneal injection) aggravated lung injury, the inflammatory response, and ferroptosis in acute lung injury (ALI) mouse model[4].

References:
[1] Huang Y, Su R, Sheng Y, et al. Small-molecule targeting of oncogenic FTO demethylase in acute myeloid leukemia. Cancer cell. 2019 Apr 15;35(4):677-91.
[2] Huang WM, Li ZX, Wu YH, et al. m6A demethylase FTO renders radioresistance of nasopharyngeal carcinoma via promoting OTUB1-mediated anti-ferroptosis. Translational oncology. 2023 Jan 1;27:101576.
[3] Xu Y, Zhou J, Li L, et al. FTO-mediated autophagy promotes progression of clear cell renal cell carcinoma via regulating SIK2 mRNA stability. International Journal of Biological Sciences. 2022;18(15):5943.
[4] Zhao Y, Ding W, Cai Y, et al. The m6A eraser FTO suppresses ferroptosis via mediating ACSL4 in LPS-induced macrophage inflammation. Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease. 2024 Oct 1;1870(7):167354.

FB23-2是一种mRNA N6-甲基腺嘌呤(M6A)脱甲基酶FTO的选择性抑制剂(IC50 = 2.6μM),可用于急性髓系白血病(AML)的研究[1]

FB23-2(72小时)对NB4和MONOMAC6细胞增殖的抑制作用的IC50分别为0.8μM和1.5μM[1]。FB23-2(10μM,96小时)能显著增强鼻咽癌(NPC)细胞对照射的敏感性[2]

FB23-2(2mg/kg/d,10天,腹腔注射)显著抑制急性髓性白血病(AML)的进展并延长AML小鼠的生存期[1]。FB23-2(8mg/kg/d,14天,腹腔注射)显著抑制透明细胞肾细胞癌(ccRCC)小鼠模型的肿瘤生长并延长小鼠的存活时间[3]。FB23-2(2mg/kg/d,3天,腹腔注射)加重了急性肺损伤(ALI)小鼠的肺损伤、炎症反应和铁死亡[4]

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Nasopharyngeal carcinoma (NPC) cells

Preparation Method

The cells (2 × 105) were seeded into dishes and cultured for 24h and treated with FB23-2 (10μmol) or transfected with Flag-FTO. After 24h, the cells were irradiated with X-ray beam at 4 Gy and were cultured again for 72h. Finally cellular lipid measurement was confirmed by flow cytometry.

Reaction Conditions

10μM, 96 hours

Applications

FB23-2 significantly sensitized NPC cells to irradiation.
Animal experiment [2]:

Animal models

Acute myeloid leukemia (AML) mouse model

Preparation Method

For the AML mouse model, 0.2 × 106 MONOMAC6 cells were directly transplanted into NOD/LtSz-scid IL2RG-SGM3 (NSGS) mice via tail vein. After 10 days, FB23-2 (2mg/kg/day) and DMSO vehicle were intraperitoneally injected into the mice for a continuous 10 days.

Dosage form

2mg/kg/d, 10 days, i.p.

Applications

FB23-2 substantially delayed the onset of full-blown leukemic symptoms and significantly prolonged survival by almost doubling the median survival.

References:
[1] Huang WM, Li ZX, Wu YH, et al. m6A demethylase FTO renders radioresistance of nasopharyngeal carcinoma via promoting OTUB1-mediated anti-ferroptosis. Translational oncology. 2023 Jan 1;27:101576.
[2] Huang Y, Su R, Sheng Y, et al. Small-molecule targeting of oncogenic FTO demethylase in acute myeloid leukemia. Cancer cell. 2019 Apr 15;35(4):677-91.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
2243736-45-8
SMILES
O=C(NO)C1=CC=CC=C1NC2=C(Cl)C=C(C3=C(C)ON=C3C)C=C2Cl
分子式
C18H15Cl2N3O3
分子量
392.24 g/mol
溶解性
DMSO: 62.5 mg/mL (159.34 mM)
保存条件
4°C, protect from light
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