ASLAN003

Catalog No.S9721 Synonyms: LAS 186323

For research use only.

ASLAN003 (LAS 186323) 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.

ASLAN003  Chemical Structure

CAS No. 1035688-66-4

Selleck's ASLAN003 has been cited by 3 Publications

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Biological Activity

Description

ASLAN003 (LAS 186323) 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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: 4-6 week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice
  • Dosages: 50 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 356.32
Formula

C19H14F2N2O3

CAS No. 1035688-66-4
Storage 3 years -20°C powder
2 years -80°C in solvent

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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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