Farudodstat
Based on 4 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.68%
- No. CAS: 1035688-66-4
- Fòrmula: C19H14F2N2O3
- Peso molecular:356.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Farudodstat
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Actividad biológica
IC50: 35 nM (human DHODH enzyme)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.7 μM
Compound: ASL; ASLAN003
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Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| A549 | IC50 |
0.9 μM
Compound: ASL; ASLAN003
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Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| HCT-116 | IC50 |
5.1 μM
Compound: ASL; ASLAN003
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Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| K562 | IC50 |
2.7 μM
Compound: ASL; ASLAN003
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Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| KG-1 | IC50 |
382 nM
Compound: ASLAN003
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Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay
Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay
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[PMID: 35151222] |
| L02 | IC50 |
486.6 nM
Compound: ASL; ASLAN003
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Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| MOLM-14 | IC50 |
582 nM
Compound: ASLAN003
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Antiproliferative activity against human MOLM-14 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay
Antiproliferative activity against human MOLM-14 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay
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[PMID: 35151222] |
| Raji | IC50 |
0.3 μM
Compound: ASL; ASLAN003
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Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| Raji | IC50 |
270 nM
Compound: ASLAN003
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Antiproliferative activity against human Raji cells assessed as cell growth inhibition measured after 96 hrs by MTT assay
Antiproliferative activity against human Raji cells assessed as cell growth inhibition measured after 96 hrs by MTT assay
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[PMID: 35640328] |
| SK-MEL-28 | IC50 |
1.3 μM
Compound: ASL; ASLAN003
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 96 hrs by MTT assay
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[PMID: 34905371] |
| THP-1 | IC50 |
152 nM
Compound: ASLAN003
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Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 48 hrs by CTG assay
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[PMID: 35151222] |
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.
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Cell Line:THP-1, MOLM-14 and KG-1 cells
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Concentration:0.01, 0.1, 1, 10, 100 μM
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Incubation Time:For 48 hours
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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.
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Cell Line:KG-1 and MOLM-14 cells
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Concentration:0.5, 1 μM
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Incubation Time:For 48 hours
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Result:Significantly increased cleaved caspase 8, increased leakage of cytochrome c from mitochondria into the cytosol and induced cleaved caspase-3 and -7.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; once daily; from the day 3 to 30
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Result:Substantially reduced the number of disseminated tumors and the size of these tumors.
Survival was significantly prolonged.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1035688-66-4
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Appearance Solid
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Peso molecular 356.32
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Fòrmula C19H14F2N2O3
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Color White to off-white
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SMILES
O=C(C1=CC=CN=C1NC2=C(F)C=C(C3=CC=CC(OC)=C3)C=C2F)O
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Synonyms
ASLAN003
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
2022 Oct:204:115232. PMID: 36030831 -
Antiviral Res
Mechanisms of antiviral activity of the new hDHODH inhibitor MEDS433 against respiratory syncytial virus replication. [Abstract]2023 Nov:219:105734. PMID: 37852322 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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