1. Apoptosis
  2. Apoptosis
  3. FB23-2

FB23-2 is a potent and selective inhibitor of mRNA N6-methyladenosine (m6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML).

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FB23-2 Chemical Structure

FB23-2 Chemical Structure

CAS No. : 2243736-45-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 15 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

FB23-2 is a potent and selective inhibitor of mRNA N6-methyladenosine (m6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML)[1].

IC50 & Target

IC50: 2.6 μM (FTO)[1]

In Vitro

FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human AML cell line cells and primary blast AML cells[1].
FB23 inhibits the proliferation of NB4 and MONOMAC6 cells, with IC50 values of 0.8 μM and 1.5 μM[1].
FB23-2 (20 μM; 72 hours) displays anti-proliferation effect via upregulating global m6A levels[1].
FB23-2 (0.5-5 μM; 24-72 hours) significantly suppresses the proliferation of BM cells from these two models in a dose-dependent manner[1].
FB23-2 exhibits FTO-dependent anti-proliferation activity and promotes myeloid differentiation and apoptosis[1].
FB23-2 (1-20 μM; 72 hours) significantly increases the mRNA and protein levels of ASB2 and RARA in NB4 and MONOMAC6 cells[1].
FB23-2 induces apoptosis (1-20 μM; 48-72 hours) and cell cycle arrest (5-20 μM; 24 hours) at G1 stage in AML cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

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[1]

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[1]

Cell Line: MONOMAC6 cells
Concentration: 5 μM , 20 μM
Incubation Time: 24 hours
Result: Induced cell cycle arrest at G1 stage.
In Vivo

FB23-2 (2 mg/kg; i.p.; daily; for 10 days) substantially suppresses leukemia progression and prolongs survival[1].
FB23-2 exhibits elimination half-life (rat 6.7 h) and Cmax (rat 2421.3 ng/mL) following intraperitoneal injection (rat 3 mg/kg)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/LtSz-scid IL2RG-SGM3 (NSGS) mice, xeno-transplanted with MONOMAC6 AML cells[1]
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[1]
Dosage: 3 mg/kg (Pharmacokinetic Analysis)
Administration: Intraperitoneal injection
Result: T1/2 (6.7 hours), Cmax (2421.3 ng/mL).
Molecular Weight

392.24

Formula

C18H15Cl2N3O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NO)C1=CC=CC=C1NC2=C(Cl)C=C(C3=C(C)ON=C3C)C=C2Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (63.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (25.49 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.93%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5495 mL 12.7473 mL 25.4946 mL 63.7365 mL
5 mM 0.5099 mL 2.5495 mL 5.0989 mL 12.7473 mL
10 mM 0.2549 mL 1.2747 mL 2.5495 mL 6.3736 mL
15 mM 0.1700 mL 0.8498 mL 1.6996 mL 4.2491 mL
20 mM 0.1275 mL 0.6374 mL 1.2747 mL 3.1868 mL
25 mM 0.1020 mL 0.5099 mL 1.0198 mL 2.5495 mL
30 mM 0.0850 mL 0.4249 mL 0.8498 mL 2.1245 mL
40 mM 0.0637 mL 0.3187 mL 0.6374 mL 1.5934 mL
50 mM 0.0510 mL 0.2549 mL 0.5099 mL 1.2747 mL
60 mM 0.0425 mL 0.2125 mL 0.4249 mL 1.0623 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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