1. Apoptosis
  2. Apoptosis
  3. FB23-2

FB23-2 

Cat. No.: HY-127103 Purity: 99.53%
Handling Instructions

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).

For research use only. We do not sell to patients.

FB23-2 Chemical Structure

FB23-2 Chemical Structure

CAS No. : 2243736-45-8

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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 205 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.
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 : 62.5 mg/mL (159.34 mM; Need ultrasonic)

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
10 mM 0.2549 mL 1.2747 mL 2.5495 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.53%

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Keywords:

FB23-2ApoptosisacutemyeloidleukemiaAMLanti-proliferationmRNAm6AdemethylaseInhibitorinhibitorinhibit

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FB23-2
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HY-127103
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