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Farudodstat

Catalog No. T10384   CAS 1035688-66-4
Synonyms: ASLAN003

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity. It has the potential to be a first-in-class candidate in AML.

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Farudodstat Chemical Structure
Farudodstat, CAS 1035688-66-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 72.00
25 mg In stock $ 155.00
50 mg In stock $ 255.00
100 mg In stock $ 411.00
1 mL * 10 mM (in DMSO) In stock $ 47.00
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Purity: 98.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity. It has the potential to be a first-in-class candidate in AML.
Targets&IC50 DHODH enzyme (human):35 nM (IC50)
In vitro ASLAN003 is a highly potent dihydroorotate dehydrogenase inhibitor that induces differentiation, as well as reduces cell proliferation and viability, of acute myeloid leukemia cell lines and primary acute myeloid leukemia blasts including in chemo-resistant cells. Apoptotic pathways are triggered by ASLAN003, and it also significantly inhibits protein synthesis and activates AP-1 transcription, contributing to its differentiation promoting capacity[2].
In vivo ASLAN003 substantially reduces leukemic burden and prolongs survival in acute myeloid leukemia xenograft mice and acute myeloid leukemia patient-derived xenograft models. Notably, the drug has no evident effect on normal hematopoietic cells and exhibits excellent safety profiles in mice, even after a prolonged period of administration. ASLAN003 is an agent targeting dihydroorotate dehydrogenase with potential in the treatment of acute myeloid leukemia. ASLAN003 is currently being evaluated in phase 2a clinical trial in acute myeloid leukemia patients[2].
Synonyms ASLAN003
Molecular Weight 356.32
Formula C19H14F2N2O3
CAS No. 1035688-66-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (336.78 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Marco L. Lolli, et al. Human Dihydroorotate Dehydrogenase (hDHODH) as a new target on Acute Myelogenous Leukemia (AML): Targeting Myeloid Differentiation using Potent and Innovative hDHODH Inhibitors. 23rd Swedish Conference on Macromolecular Structure and Function Tällberg, 14-17 June 2019 2. Jianbiao Zhou, et al. ASLAN003, a potent dihydroorotate dehydrogenase inhibitor for differentiation of acute myeloid leukemia. Haematologica. 2019 Nov7;haematol.2019.230482.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Preclinical Compound Library Mitochondria-Targeted Compound Library Bioactive Compounds Library Max Anti-Infection Compound Library Clinical Compound Library

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Keywords

Farudodstat 1035688-66-4 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Dehydrogenase DNA/RNA Synthesis AML RPL6 synthesis OPP acute protein orally EIF4B myeloid caspase-3 DHODH caspase-7 THP-1 AP-1 caspase-8 MOLM-14 ASLAN-003 inhibit ASLAN003 KG-1 leukemia Inhibitor ASLAN 003 Dihydroorotate Dehydrogenase inhibitor

 

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