DHODH-IN-21
DHODH-IN-21 (compound 19) is an orally active selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 1.1 nM. DHODH-IN-21 has anticancer activity and can be used in studies of acute myeloid leukaemia (AML).
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- No. CAS: 2450341-39-4
- Fòrmula: C20H19ClF4N6O4
- Peso molecular:518.85
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Mouse DHODH 140 nM (IC50) |
Rat DHODH 1580 nM (IC50) |
Dog DHODH 8.5 nM (IC50) |
Monkey DHODH 1.6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MOLM-13 | IC50 |
2 nM
Compound: 19
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Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 35925768] |
| THP-1 | IC50 |
5 nM
Compound: 19
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Antiproliferative activity against human THP-1 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human THP-1 cells assessed as reduction in cell viability measured after 72 hrs
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[PMID: 35925768] |
In Vitro
DHODH-IN-21 (compound 19) inhibits the proliferation of MOLM-13 and THP-1 cells with the IC50 values of 2.0 nM and 5.0 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human MOLM-13 AML xenograft model in female NSG mice[1]
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Dosage:10, 20 mg/kg
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Administration:Oral administration; everyday; 5 days
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Result:Inhibited tumor volume size by 44% and 60% at 10 mg/kg and 20 mg/kg respectively.
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Animal Model:Mouse, rat[1]
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Dosage:
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Administration:2 mg/kg i.v. or 10 mg/kg p.o.
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Result:The pharmacokinetic parameters of DHODH-IN-21 (compound 19)
Parameter Mouse Rat CL (mL/min/kg) 11 32 Vdss (L/kg) 1.3 2.3 t1/2(h) 2.3 2.0 Cmax (ng/mL) 4047 1713 tmax(h) 0.42 1.7 AUC0→inf(h•ng/mL) 16,066 9214 F% 103 167
Chemical Information
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No. CAS 2450341-39-4
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Peso molecular 518.85
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Fòrmula C20H19ClF4N6O4
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SMILES
O=C1N(C2=C(F)C=C(C(NC3=C(Cl)N=CC=C3C)=O)C(O[C@@H](C)C(F)(F)F)=N2)N=C(N1CC)CO
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DHODH-IN-21 Related Classifications
HY-149030 Related Classifications
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