Art. -Nr.: HY-129239

Farudodstat

(Synonyms: ASLAN003)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC₅₀ of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.68%
CAS. Nr.: 1035688-66-4
Formel: C₁₉H₁₄F₂N₂O₃
Molecular Weight:356.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Farudodstat Chemical Structure

CAS. Nr.: 1035688-66-4

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 35 nM (human DHODH enzyme)^[1]

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.7 μM Compound: ASL; ASLAN003	Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
A549	IC₅₀	0.9 μM Compound: ASL; ASLAN003	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
HCT-116	IC₅₀	5.1 μM Compound: ASL; ASLAN003	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
K562	IC₅₀	2.7 μM Compound: ASL; ASLAN003	Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
KG-1	IC₅₀	382 nM Compound: ASLAN003	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay	[PMID: 35151222]
L02	IC₅₀	486.6 nM Compound: ASL; ASLAN003	Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
MOLM-14	IC₅₀	582 nM Compound: ASLAN003	Antiproliferative activity against human MOLM-14 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay Antiproliferative activity against human MOLM-14 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay	[PMID: 35151222]
Raji	IC₅₀	0.3 μM Compound: ASL; ASLAN003	Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
Raji	IC₅₀	270 nM Compound: ASLAN003	Antiproliferative activity against human Raji cells assessed as cell growth inhibition measured after 96 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as cell growth inhibition measured after 96 hrs by MTT assay	[PMID: 35640328]
SK-MEL-28	IC₅₀	1.3 μM Compound: ASL; ASLAN003	Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay	[PMID: 34905371]
THP-1	IC₅₀	152 nM Compound: ASLAN003	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay	[PMID: 35151222]

In Vitro

Farudodstat (0.01-100 μM; for 48 hours) inhibits leukemic cell proliferation. The cell viability is maintained at ~50% at Farudodstat 1 μM and higher^[1].
Farudodstat (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8^[1].
Farudodstat (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples^[1].
Farudodstat (1, 2 μM; pretreatment 1 h before OPP for 1 h) inhibits protein synthesis, as demonstrated by the reduced incorporation of O-propargyl-puromycin (OPP) at protein translation sites in both MOLM-14 and KG-1 cells. Farudodstat causes the downregulation of EIF4B, and RPL6 proteins^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

THP-1, MOLM-14 and KG-1 cells
Concentration:

0.01, 0.1, 1, 10, 100 μM
Incubation Time:

For 48 hours
Result:

Inhibited leukemic cell proliferation of THP-1, MOLM-14 and KG-1 with IC₅₀ values of 152 nM, 582 nM, and 382 nM, respectively.

Western Blot Analysis^[1]

Cell Line:

KG-1 and MOLM-14 cells
Concentration:

0.5, 1 μM
Incubation Time:

For 48 hours
Result:

Significantly increased cleaved caspase 8, increased leakage of cytochrome c from mitochondria into the cytosol and induced cleaved caspase-3 and -7.

In Vivo

Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival^[1].

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

Animal Model:

Female NOD.Cg-Prkdc^scid Il2rg^tm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells^[1]
Dosage:

50 mg/kg
Administration:

Oral gavage; once daily; from the day 3 to 30
Result:

Substantially reduced the number of disseminated tumors and the size of these tumors.
Survival was significantly prolonged.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1035688-66-4
Appearance Solid
Molecular Weight 356.32
Formel C₁₉H₁₄F₂N₂O₃
Color White to off-white
SMILES

O=C(C1=CC=CN=C1NC2=C(F)C=C(C3=CC=CC(OC)=C3)C=C2F)O
Synonyms

ASLAN003
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

All

Sort by:

Journal Impact Factor

Biochem Pharmacol

IMP075 targeting ClpP for colon cancer therapy in vivo and in vitro. [Abstract]

2022 Oct:204:115232. PMID: 36030831
Antiviral Res

Mechanisms of antiviral activity of the new hDHODH inhibitor MEDS433 against respiratory syncytial virus replication. [Abstract]

2023 Nov:219:105734. PMID: 37852322
bioRxiv

2026 Jan 27.
Res Sq

2025 Sep 14.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (350.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8065 mL

14.0323 mL

28.0647 mL

5 mM

0.5613 mL

2.8065 mL

5.6129 mL

10 mM

0.2806 mL

1.4032 mL

2.8065 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.17 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.

Protocol 2

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

Solubility: ≥ 2.17 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 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 (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jianbiao Zhou, et al. ASLAN003, a potent dihydroorotate dehydrogenase inhibitor for differentiation of acute myeloid leukemia. Haematologica. 2019 Nov7;haematol.2019.230482.

[2]. Marco L. Lolli, et al. Human Dihydroorotate Dehydrogenase (hDHODH) as a new target on Acute Myelogenous Leukemia (AML): Targeting Myeloid Differentiation using Potent and Innovative hDHODH Inhibitors. 23rd Swedish Conference on Macromolecular Structure and Function Tällberg, 14-17 June 2019

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8065 mL	14.0323 mL	28.0647 mL	70.1617 mL
	5 mM	0.5613 mL	2.8065 mL	5.6129 mL	14.0323 mL
	10 mM	0.2806 mL	1.4032 mL	2.8065 mL	7.0162 mL
	15 mM	0.1871 mL	0.9355 mL	1.8710 mL	4.6774 mL
	20 mM	0.1403 mL	0.7016 mL	1.4032 mL	3.5081 mL
	25 mM	0.1123 mL	0.5613 mL	1.1226 mL	2.8065 mL
	30 mM	0.0935 mL	0.4677 mL	0.9355 mL	2.3387 mL
	40 mM	0.0702 mL	0.3508 mL	0.7016 mL	1.7540 mL
	50 mM	0.0561 mL	0.2806 mL	0.5613 mL	1.4032 mL
	60 mM	0.0468 mL	0.2339 mL	0.4677 mL	1.1694 mL
	80 mM	0.0351 mL	0.1754 mL	0.3508 mL	0.8770 mL
	100 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7016 mL

Farudodstat

4 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Farudodstat

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Ferroptosis Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Farudodstat

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Farudodstat

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Ferroptosis Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Farudodstat

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Farudodstat Related Classifications

HY-129239 Related Classifications