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%
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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.

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Farudodstat Chemical Structure

Farudodstat Chemical Structure

CAS No. : 1035688-66-4

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Farudodstat Related Antibodies

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  • Purity & Documentation

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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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (350.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.70%

COA (248 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8065 mL 14.0323 mL 28.0647 mL 70.1617 mL
5 mM 0.5613 mL 2.8065 mL 5.6129 mL 14.0323 mL
10 mM 0.2806 mL 1.4032 mL 2.8065 mL 7.0162 mL
15 mM 0.1871 mL 0.9355 mL 1.8710 mL 4.6774 mL
20 mM 0.1403 mL 0.7016 mL 1.4032 mL 3.5081 mL
25 mM 0.1123 mL 0.5613 mL 1.1226 mL 2.8065 mL
30 mM 0.0935 mL 0.4677 mL 0.9355 mL 2.3387 mL
40 mM 0.0702 mL 0.3508 mL 0.7016 mL 1.7540 mL
50 mM 0.0561 mL 0.2806 mL 0.5613 mL 1.4032 mL
60 mM 0.0468 mL 0.2339 mL 0.4677 mL 1.1694 mL
80 mM 0.0351 mL 0.1754 mL 0.3508 mL 0.8770 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7016 mL
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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.

Keywords:

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

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