DHODH-IN-22
DHODH-IN-22 is a potent, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 0.3 nM. DHODH-IN-22 can be used for researching acute myelogenous leukemia (AML).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2450341-75-8
- Formel: C21H21ClF4N6O5
- Molecular Weight:548.88
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
IC50: 0.3 nM (human DHODH), 10 nM (mouse DHODH), 130 nM (rat DHODH), 4.2 nM (dog DHODH), 0.54 nM (monkey DHODH)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
0.4 nM
Compound: 29
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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] |
| MOLM-13 | IC50 |
0.4 nM
Compound: Fig 1, Cpd 2
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Antiproliferative activity in human MOLM-13 AML cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity in human MOLM-13 AML cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 38505861] |
| THP-1 | IC50 |
1.4 nM
Compound: 29
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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] |
DHODH-IN-22 (compound 29) exhibits antiproliferative activity against MOLM-13 and THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13 and THP-1
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Concentration:0-30 nM
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Incubation Time:72 h
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Result:Exhibited antiproliferative activity against MOLM-13 and THP-1 cells with IC50s of 0.4 nM and 1.4 nM, respectively.
DHODH-IN-22 (2 mg/kg for IV and 10 mg/kg for PO; single dosage) has favorable pharmacokinetic property[1].
Pharmacokinetic Parameters of DHODH-IN-22 (compound 29) in mouse and rat[1].
| Mouse IV 2 mg/kg and PO 10 mg/kg |
Rat IV 2 mg/kg and PO 10 mg/kg |
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| CL (mL/min/kg) | 7.3 | 7.6 |
| Vdss (L/kg) | 2.4 | 2.2 |
| t1/2 (ng/mL) | 5 | 4 |
| Cmax (ng/mL) | 3810 | 2193 |
| tmax (h) | 1.0 | 4.0 |
| AUC0-inf (ng/mL·h) | 23046 | 23807 |
| F (%) | 110 | 106 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NSG mice (implanted subcutaneously with 2 × 106 MOLM-13 tumor cells)[1]
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Dosage:1.9, 3.75 and 7.5 mg/kg
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Administration:PO; QD for 5 days
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Result:Significantly inhibited tumor growth with ΔTGI% of 71, 76, and 79% at 1.9, 3.75 and 7.5 mg/kg, respectively, and exhibited no significant impact on body weight over the course of 5 days.
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Animal Model:Rat and mouse[1]
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Dosage:2 mg/kg IV and 10 mg/kg PO
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Administration:IV or PO; single dosage (Pharmacokinetic analysis)
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Result:Exhibited low clearance and high oral bioavailability in both species.
Chemical Information
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CAS. Nr. 2450341-75-8
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Molecular Weight 548.88
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Formel C21H21ClF4N6O5
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SMILES
O=C(C1=CC(F)=C(N2N=C(CO)N(CC)C2=O)N=C1O[C@@H](C)C(F)(F)F)NC3=C(Cl)C(OC)=NC=C3C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
DHODH-IN-22 Related Classifications
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