Farudodstat

Catalog No.S9721 Batch:S972101

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Technical Data

Formula

C19H14F2N2O3
Molecular Weight 356.32 CAS No. 1035688-66-4
Solubility (25°C)* In vitro DMSO 71 mg/mL (199.25 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.88mg/ml (2.47mM) Taking the 1 mL working solution as an example, add 50 μL of 17.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.5mg/ml (1.40mM) Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 Assay:

[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 Study:

[1]
  • Animal Models

    4-6 week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice

  • Dosages

    50 mg/kg

  • Administration

    Oral gavage

Selleck's Farudodstat has been cited by 4 publications

Selective vulnerability of human-induced pluripotent stem cells to dihydroorotate dehydrogenase inhibition during mesenchymal stem/stromal cell purification [ Front Cell Dev Biol, 2023, 11:1089945] PubMed: 36814599
Inhibitors of dihydroorotate dehydrogenase cooperate with molnupiravir and N4-hydroxycytidine to suppress SARS-CoV-2 replication [ iScience, 2022, 25(5):104293] PubMed: 35492218
N4-hydroxycytidine and inhibitors of dihydroorotate dehydrogenase synergistically suppress SARS-CoV-2 replication [ bioRxiv, 2021, 10.1101/2021.06.28.450163] PubMed: N/A
N4-hydroxycytidine and inhibitors of dihydroorotate dehydrogenase synergistically suppress SARS-CoV-2 replication [ bioRxiv, 2021, 10.1101/2021.06.28.450163] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.