FNDR-20123 free base

Cat. No.: HY-131708: FAQs
Data Sheet Handling Instructions

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FNDR-20123 free base 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 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC₅₀=41 nM) and sexual blood stage (IC₅₀=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC₅₀=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations.

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

FNDR-20123 free base Chemical Structure

CAS No. : 1267502-34-0

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Other In-stock Forms of FNDR-20123 free base:

Other Forms of FNDR-20123 free base:

FNDR-20123 In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

Plasmodium

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].

MedChemExpress (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].

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

Animal Model:	P. falciparum Pf3D^70087/N9 in NODscidIL2Rγ^null 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

377.44

Formula

C₂₁H₂₃N₅O₂

CAS No.

1267502-34-0

SMILES

O=C(NO)C1=CC=C(CN2N=NC(C3=CC=C(CN4CCCC4)C=C3)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 35.71 mg/mL (94.61 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	2.6494 mL	13.2471 mL	26.4943 mL
5 mM	0.5299 mL	2.6494 mL	5.2989 mL
10 mM	0.2649 mL	1.3247 mL	2.6494 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 (5.51 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.51 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.51 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(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).

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

Handling Instructions (2659 KB)

References

[1]. Potluri V, et al. Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J. 2020;19(1):365. Published 2020 Oct 12. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6494 mL	13.2471 mL	26.4943 mL	66.2357 mL
	5 mM	0.5299 mL	2.6494 mL	5.2989 mL	13.2471 mL
	10 mM	0.2649 mL	1.3247 mL	2.6494 mL	6.6236 mL
	15 mM	0.1766 mL	0.8831 mL	1.7663 mL	4.4157 mL
	20 mM	0.1325 mL	0.6624 mL	1.3247 mL	3.3118 mL
	25 mM	0.1060 mL	0.5299 mL	1.0598 mL	2.6494 mL
	30 mM	0.0883 mL	0.4416 mL	0.8831 mL	2.2079 mL
	40 mM	0.0662 mL	0.3312 mL	0.6624 mL	1.6559 mL
	50 mM	0.0530 mL	0.2649 mL	0.5299 mL	1.3247 mL
	60 mM	0.0442 mL	0.2208 mL	0.4416 mL	1.1039 mL
	80 mM	0.0331 mL	0.1656 mL	0.3312 mL	0.8279 mL