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FB23-2 FTO inhibitor

Cat.No.S8837

FB23-2 is a potent and selective FTO inhibitor that directly binds to FTO and selectively inhibits this compound's N6-methyladenosine (m6A) demethylase activity with IC50 of 2.6 μM.
FB23-2 FTO inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 392.24

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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (198.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 392.24 Formula

C18H15Cl2N3O3

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2243736-45-8 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C(=NO1)C)C2=CC(=C(C(=C2)Cl)NC3=CC=CC=C3C(=O)NO)Cl

Mechanism of Action

Targets/IC50/Ki
FTO
(Cell-free assay)
2.6 μM
In vitro

FB23-2 directly binds to FTO and selectively inhibits its m6A demethylase activity. Mimicking FTO depletion, this compound dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro.

In vivo

FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice.

References

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