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: 1035688-66-4

Selleck's Farudodstat has been cited by 4 publications

Purity & Quality Control

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

Farudodstat Related Products

Choose Selective Dehydrogenase Inhibitors

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Farudodstat | Farudodstat supplier | purchase Farudodstat | Farudodstat cost | Farudodstat manufacturer | order Farudodstat | Farudodstat distributor