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).
For research use only. We do not sell to patients.
- CAS No.: 2450341-75-8
- Formula: C21H21ClF4N6O5
- Molecular Weight:548.88
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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]
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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 No. 2450341-75-8
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Molecular Weight 548.88
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DHODH-IN-22 Related Classifications
HY-149031 Related Classifications
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