FB23-2

SKU: orb1225610

Description

FB23-2 is a potent, selective inhibitor of the mRNA N 6-methyladenosine (m 6A) demethylase FTO, directly bind to FTO, inhibits FTO demethylation of m6 A in RNA in vitro with IC50 of 2.6 uM; demonstrates significantly improved anti-proliferative activity on NB4 and MONOMAC6 cells with IC50 of 0.8-1.5 uM, compared with parental compound FB23; dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro; FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice.

Key Properties

• CAS Number: 2243736-45-8
• MW: 392.236
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₅Cl₂N₃O₃
• SMILES: O=C(NO)C1=CC=CC=C1NC2=C(Cl)C=C(C3=C(C)ON=C3C)C=C2Cl
• Target: Histone Demethylase
• Solubility: DMSO : 62.5 mg/mL 159.34 mM

Bioactivity

• In Vivo:
  Animal model: NOD/LtSz-scid IL2RG-SGM3 (NSGS) mice, xeno-transplanted with MONOMAC6 AML cells. Dosage: 2 mg/kg. Administration: Intraperitoneal injection, daily, for 10 days. Result: Delayed the onset of full-blown leukemic symptoms and significantly prolonged survival by almost doubling the median survival. Animal model: Sprague Dawley (SD) rats. Dosage: 3 mg/kg (Pharmacokinetic Analysis). Administration: Intraperitoneal injection. Result: T1/2 (6.7 hours), Cmax (2421.3 ng/mL).
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• In Vitro:
  Cell Proliferation Assay Cell line: MA9 cells, FLT3ITD/NPM1 cells (mouse BM cells). Concentration: 0.5 μM, 2 μM, 5 μM Incubation time: 24 hours, 48 hours, 72 hours. Result: Suppressed the proliferation of BM cells. RT-PCR Cell line: NB4 cells, MONOMAC6 cells. Concentration: 1 μM, 5 μM, 20 μM. Incubation time: 72 hours. Result: Significantly increased ASB2 and RARA mRNA levels. Apoptosis Analysis Cell line: NB4 cells, MONOMAC6 cells. Concentration: 1 μM, 5 μM, 20 μM. Incubation time: 48 hours (NB4 cells), 72 hours (MONOMAC6 cells). Result: Induced apoptosis. Cell Cycle Analysis Cell line: MONOMAC6 cells. Concentration: 5 μM, 20 μM. Incubation time: 24 hours. Result: Induced cell cycle arrest at G1 stage.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FTO Demethylase inhibitor FB23-2

Quick Database Links

Gene Symbol

Histone Demethylase