1. Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
    Apoptosis
  2. Dihydroorotate Dehydrogenase
    DNA/RNA Synthesis
    Apoptosis
  3. ASLAN003

ASLAN003 

Cat. No.: HY-129239 Purity: 99.95%
Handling Instructions

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.

For research use only. We do not sell to patients.

ASLAN003 Chemical Structure

ASLAN003 Chemical Structure

CAS No. : 1035688-66-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 274 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 990 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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[1][2].

IC50 & Target

IC50: 35 nM (human DHODH enzyme)[1]

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[1].
ASLAN003 (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8[1].
ASLAN003 (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: THP-1, MOLM-14 and KG-1 cells
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: For 48 hours
Result: Inhibited leukemic cell proliferation of THP-1, MOLM-14 and KG-1 with IC50 values of 152 nM, 582 nM, and 382 nM, respectively.

Western Blot Analysis[1]

Cell Line: KG-1 and MOLM-14 cells
Concentration: 0.5, 1 μM
Incubation Time: For 48 hours
Result: Significantly increased cleaved caspase 8, increased leakage of cytochrome c from mitochondria into the cytosol and induced cleaved caspase-3 and -7.
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells[1]
Dosage: 50 mg/kg
Administration: Oral gavage; once daily; from the day 3 to 30
Result: Substantially reduced the number of disseminated tumors and the size of these tumors.
Survival was significantly prolonged.
Clinical Trial
Molecular Weight

356.32

Formula

C₁₉H₁₄F₂N₂O₃

CAS No.

1035688-66-4

SMILES

O=C(C1=CC=CN=C1NC2=C(F)C=C(C3=CC=CC(OC)=C3)C=C2F)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 130 mg/mL (364.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8065 mL 14.0323 mL 28.0647 mL
5 mM 0.5613 mL 2.8065 mL 5.6129 mL
10 mM 0.2806 mL 1.4032 mL 2.8065 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (6.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (6.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ASLAN003ASLAN 003ASLAN-003Dihydroorotate DehydrogenaseDNA/RNA SynthesisApoptosisDHODHorallyproteinsynthesisAP-1acutemyeloidleukemiaAMLTHP-1MOLM-14KG-1EIF4BRPL6OPPO-propargyl-puromycincaspase-8caspase-3caspase-7Inhibitorinhibitorinhibit

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ASLAN003
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HY-129239
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