Farudodstat

SKU: orb1309976

Description

Farudodstat (ASLAN003) is a potent, orally bioavailable inhibitor of human dihydroorotate dehydrogenase (DHODH) with demonstrated antitumor activity. It shows promise as a first-in-class therapeutic candidate for acute myeloid leukemia (AML), supported by evidence from both in vitro cellular assays and in vivo animal models.

Research Area

Cell Biology, Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 1035688-66-4
• MW: 356.32
• Purity: 98.03% (May vary between batches)
• Formula: C₁₉H₁₄F₂N₂O₃
• SMILES: COc1cccc(c1)-c1cc(F)c(Nc2ncccc2C(O)=O)c(F)c1
• Target: DNA/RNA Synthesis|||Apoptosis|||Dehydrogenase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.23 mM);DMSO:250 mg/mL (701.62 mM)

Bioactivity

• Target IC50:
  DHODH enzyme (human):35 nM (IC50)
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DHODH, Dihydroorotate Dehydrogenase, DNASynthesis, DNA/RNA Synthesis, DNA Synthesis, acute, ASLAN 003, ASLAN003, ASLAN-003, AP-1, Apoptosis, AML, caspase-8, caspase-7, caspase-3, MOLM-14, OPP, orally, KG-1, inhibit, myeloid, Inhibitor, leukemia, EIF4B, Farudodstat, RPL6, RNASynthesis, RNA Synthesis, synthesis, protein, THP-1

Compound Identifiers

PubChem CID

24986824