Description
ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
Product information
CAS Number: 1035688-66-4
Molecular Weight: 356.32
Formula: C19H14F2N2O3
Chemical Name: 2-({3,5-difluoro-3'-methoxy-[1,1'-biphenyl]-4-yl}amino)pyridine-3-carboxylic acid
Smiles: COC1=CC(=CC=C1)C1=CC(F)=C(NC2=NC=CC=C2C(O)=O)C(F)=C1
InChiKey: OMPATGZMNFWVOH-UHFFFAOYSA-N
InChi: InChI=1S/C19H14F2N2O3/c1-26-13-5-2-4-11(8-13)12-9-15(20)17(16(21)10-12)23-18-14(19(24)25)6-3-7-22-18/h2-10H,1H3,(H,22,23)(H,24,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 130 mg/mL (364.84 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ASLAN003 (0.01-100 μM; for 48 hours) inhibits leukemic cell proliferation. The cell viability is maintained at ~50% at ASLAN003 1 μM and higher. ASLAN003 (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8. ASLAN003 (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples. ASLAN003 (1, 2 μM; pretreatment 1 h before OPP for 1 h) inhibits protein synthesis, as demonstrated by the reduced incorporation of O-propargyl-puromycin (OPP) at protein translation sites in both MOLM-14 and KG-1 cells. ASLAN003 causes the downregulation of EIF4B, and RPL6 proteins.
In Vivo:
ASLAN003 (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival.
Products are for research use only. Not for human use.
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