1. Metabolic Enzyme/Protease
  2. Dihydroorotate Dehydrogenase
  3. 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.

DHODH-IN-22 Chemical Structure

DHODH-IN-22 Chemical Structure

CAS No. : 2450341-75-8

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Description

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)[1].

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]

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.

Cell Proliferation Assay[1]

Cell Line: MOLM-13 and THP-1
Concentration: 0-30 nM
Incubation Time: 72 h
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 (1.9-7.5 mg/kg; PO; QD for 5 days) significantly inhibits MOLM-13 tumor growth in mice, and exhibits no significant impact on body weight[1].
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
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.

Animal Model: Female NSG mice (implanted subcutaneously with 2 × 106 MOLM-13 tumor cells)[1]
Dosage: 1.9, 3.75 and 7.5 mg/kg
Administration: PO; QD for 5 days
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.
Animal Model: Rat and mouse[1]
Dosage: 2 mg/kg IV and 10 mg/kg PO
Administration: IV or PO; single dosage (Pharmacokinetic analysis)
Result: Exhibited low clearance and high oral bioavailability in both species.
Molecular Weight

548.88

Formula

C21H21ClF4N6O5

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
DHODH-IN-22
Cat. No.:
HY-149031
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