FB23-2
目录号 : GC36032
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。
Cas No.:2243736-45-8
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
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Cell lines |
Nasopharyngeal carcinoma (NPC) cells |
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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]: | |
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Animal models |
Acute myeloid leukemia (AML) mouse model |
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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: |
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| Cas No. | 2243736-45-8 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO: 62.5 mg/mL (159.34 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5495 mL | 12.7473 mL | 25.4946 mL |
| 5 mM | 0.5099 mL | 2.5495 mL | 5.0989 mL |
| 10 mM | 0.2549 mL | 1.2747 mL | 2.5495 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet