1. Cell Cycle/DNA Damage
    Epigenetics
    Anti-infection
  2. HDAC
    Parasite
  3. FNDR-20123

FNDR-20123 

Cat. No.: HY-131708A Purity: 98.08%
Handling Instructions

FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations.

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

FNDR-20123 Chemical Structure

FNDR-20123 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 418 In-stock
Estimated Time of Arrival: December 31
5 mg USD 380 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of FNDR-20123:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations[1].

IC50 & Target[1]

human HDAC

3 nM (IC50)

Plasmodium HDAC

31 nM (IC50)

HDAC1

25 nM (IC50)

HDAC2

29 nM (IC50)

HDAC3

2 nM (IC50)

HDAC6

11 nM (IC50)

HDAC8

282 nM (IC50)

In Vitro

FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite[1].

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

In Vivo

FNDR-20123 (10-50 mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection[1].

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

Animal Model: P. falciparum Pf3D70087/N9 in NODscidIL2Rγnull mice (engrafted with human erythrocytes)[1]
Dosage: 10 and 50 mg/kg
Administration: P.o.; bw for 4 days
Result: Resulted in a significant reduction in parasitaemia with 6.5% and 2.57% parasitaemia at 10 and 50 mg/kg, respectively.
Molecular Weight

413.90

Formula

C₂₁H₂₄ClN₅O₂

SMILES

O=C(NO)C1=CC=C(CN2N=NC(C3=CC=C(CN4CCCC4)C=C3)=C2)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (75.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4160 mL 12.0802 mL 24.1604 mL
5 mM 0.4832 mL 2.4160 mL 4.8321 mL
10 mM 0.2416 mL 1.2080 mL 2.4160 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 (5.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.03 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.03 mM); Clear solution

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

Purity: 98.08%

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Keywords:

FNDR-20123FNDR20123FNDR 20123HDACParasiteHistone deacetylasesresistantstrainsMDRsafeasexualmalegametocytesInhibitorinhibitorinhibit

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Product Name:
FNDR-20123
Cat. No.:
HY-131708A
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