2. Metabolic Enzyme/Protease
  3. Dihydroorotate Dehydrogenase
  4. 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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DHODH-IN-21 Chemical Structure

DHODH-IN-21 Chemical Structure

CAS No. : 2450341-39-4

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DHODH-IN-21 Related Antibodies

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Description

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)[1].

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
Cell Line Type Value Description References
MOLM-13 IC50
2 nM
Compound: 19
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
[PMID: 35925768]
THP-1 IC50
5 nM
Compound: 19
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
[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.

DHODH-IN-21 Related Antibodies
In Vivo

DHODH-IN-21 (compound 19) (p.o., 10 or 20 mg/kg, everyday, 5 days) inhibits tumor growth in a dose-dependent manner but no effect on body weight in female NSG mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Human MOLM-13 AML xenograft model in female NSG mice[1]
Dosage: 10, 20 mg/kg
Administration: Oral administration; everyday; 5 days
Result: Inhibited tumor volume size by 44% and 60% at 10 mg/kg and 20 mg/kg respectively.
Animal Model: Mouse, rat[1]
Dosage:
Administration: 2 mg/kg i.v. or 10 mg/kg p.o.
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
Molecular Weight

518.85

Formula

C20H19ClF4N6O4
CAS No.
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
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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DHODH-IN-21 Related Classifications

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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.

Keywords:

DHODH-IN-212450341-39-4Dihydroorotate DehydrogenaseDHODHDHODH inhibitordihydroorotate dehydrogenaseanticanceracute myeloid leukaemiaAMLInhibitorinhibitorinhibit

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