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

Farudodstat  (Synonyms: ASLAN003)

Cat. No.: HY-129239 Purity: 99.70%
COA Handling Instructions

Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.

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

Farudodstat Chemical Structure

Farudodstat Chemical Structure

CAS No. : 1035688-66-4

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10 mM * 1 mL in DMSO USD 60 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Farudodstat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Farudodstat

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  • References

  • Customer Review

Description

Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat 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

Farudodstat (0.01-100 μM; for 48 hours) inhibits leukemic cell proliferation. The cell viability is maintained at ~50% at Farudodstat 1 μM and higher[1].
Farudodstat (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8[1].
Farudodstat (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples[1].
Farudodstat (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. Farudodstat causes the downregulation of EIF4B, and RPL6 proteins[1].

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

Farudodstat Related Antibodies

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

Farudodstat (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

Appearance

Solid

Formula

C19H14F2N2O3
CAS No.
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 : 125 mg/mL (350.81 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 available by MCE.
Purity & Documentation

Purity: 99.70%

COA (247 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References
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Farudodstat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Farudodstat1035688-66-4ASLAN003ASLAN 003ASLAN-003Dihydroorotate DehydrogenaseDNA/RNA SynthesisApoptosisDHODHorallyproteinsynthesisAP-1acutemyeloidleukemiaAMLTHP-1MOLM-14KG-1EIF4BRPL6OPPO-propargyl-puromycincaspase-8caspase-3caspase-7Inhibitorinhibitorinhibit

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