ASLAN003

For research use only.

Catalog No.S9721 Synonyms: LAS 186323

1 publication

ASLAN003  Chemical Structure

CAS No. 1035688-66-4

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.

Selleck's ASLAN003 has been cited by 1 publication

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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]
()
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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.25 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.32
Formula

C19H14F2N2O3

CAS No. 1035688-66-4
Storage powder
in solvent
Synonyms LAS 186323

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID