Home Metabolism Dehydrogenase inhibitor - Apoptosis related activator - AP-1 agonist Farudodstat For research use only.

Farudodstat

Synonyms: LAS 186323,ASLAN003

Farudodstat(LAS 186323,ASLAN003) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors.

Farudodstat Chemical Structure

Farudodstat Chemical Structure

CAS No. 1035688-66-4

Purity & Quality Control

Batch: S972101 DMSO]71 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.9%
99.9

Farudodstat Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Biological Activity

Description

Farudodstat(LAS 186323,ASLAN003) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors.
Targets
AP-1 [1] AP-1 [1] human DHODH [1]
(Cell-free assay)
35 nM
In vitro
In vitro

ASLAN003 is a highly potent dihydroorotate dehydrogenase inhibitor that induces differentiation, as well as reducing cell proliferation and viability, of AML cell lines and primary AML blasts including chemoresistant cells. Apoptotic pathways are triggered by ASLAN003, and this drug also significantly inhibits protein synthesis and activates AP-1 transcription, contributing to its capacity to promote differentiation.[1]
Cell Research Cell lines MOLM-14 cells, KG-1 cells
Concentrations 1 μM, 2 μM
Incubation Time 1 h
Method

Click-iT assays are performed using an O-propargylpuromycin (OPP) Alexa Fluor® 488 Protein Synthesis Assay Kit according to the manufacturer’s recommendation. MOLM-14 and KG-1 cells are exposed to ASLAN003 1 μM or 2 μM for 1 h before OPP 20 mM was added for 1 h. DMSO is used as a control. Cells are washed in ice-cold phosphate-buffered saline and then fixed and permeabilized prior to FACS analysis using a LSRII flow cytometer.
In Vivo
In vivo

ASLAN003 substantially reduces leukemic burden and prolongs survival in AML xenograft mice and AML patient-derived xenograft models. ASLAN003 has no evident effect on normal hematopoietic cells and exhibits excellent safety profiles in mice, even after a prolonged period of administration.[1]
Animal Research Animal Models 4-6 week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice
Dosages 50 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 356.32 Formula

C19H14F2N2O3
CAS No. 1035688-66-4 SDF --
Smiles COC1=CC=CC(=C1)C2=CC(=C(NC3=NC=CC=C3C(O)=O)C(=C2)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (199.25 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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