产品
编 号：F752856
分子式：C20H19ClF4N6O4
分子量：518.85
分子式：C20H19ClF4N6O4
分子量：518.85
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CAS No: 2450341-39-4
产品详情
生物活性：
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).
体内研究：
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.Animal Model:Human MOLM-13 AML xenograft model in female NSG mice
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
Dosage:
Administration:2 mg/kg i.v. or 10 mg/kg p.o.
Result:The pharmacokinetic parameters of DHODH-IN-21 (compound 19)ParameterMouseRat
CL (mL/min/kg)1132
Vdss (L/kg)1.32.3
t1/2(h)2.32.0
Cmax (ng/mL)40471713
tmax(h)0.421.7
AUC0→inf(h?ng/mL)16,0669214
F%103167
体外研究：
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.
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).
体内研究：
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.Animal Model:Human MOLM-13 AML xenograft model in female NSG mice
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
Dosage:
Administration:2 mg/kg i.v. or 10 mg/kg p.o.
Result:The pharmacokinetic parameters of DHODH-IN-21 (compound 19)ParameterMouseRat
CL (mL/min/kg)1132
Vdss (L/kg)1.32.3
t1/2(h)2.32.0
Cmax (ng/mL)40471713
tmax(h)0.421.7
AUC0→inf(h?ng/mL)16,0669214
F%103167
体外研究：
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.
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