产品
编 号：F752857
分子式：C21H21ClF4N6O5
分子量：548.88
分子式：C21H21ClF4N6O5
分子量：548.88
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CAS No: 2450341-75-8
产品详情
生物活性：
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).
体内研究：
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.DHODH-IN-22 (2 mg/kg for IV and 10 mg/kg for PO; single dosage) has favorable pharmacokinetic property.Pharmacokinetic Parameters of DHODH-IN-22 (compound 29) in mouse and rat.MouseIV 2 mg/kg and PO 10 mg/kg RatIV 2 mg/kg and PO 10 mg/kg
CL (mL/min/kg)7.37.6
Vdss (L/kg)2.42.2
t1/2 (ng/mL)54
Cmax (ng/mL)38102193
tmax (h)1.04.0
AUC0-inf (ng/mL·h)2304623807
F (%)110106
Animal Model:Female NSG mice (implanted subcutaneously with 2 × 106 MOLM-13 tumor cells)
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
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.
体外研究：
DHODH-IN-22 (compound 29) exhibits antiproliferative activity against MOLM-13 and THP-1 cells.
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).
体内研究：
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.DHODH-IN-22 (2 mg/kg for IV and 10 mg/kg for PO; single dosage) has favorable pharmacokinetic property.Pharmacokinetic Parameters of DHODH-IN-22 (compound 29) in mouse and rat.MouseIV 2 mg/kg and PO 10 mg/kg RatIV 2 mg/kg and PO 10 mg/kg
CL (mL/min/kg)7.37.6
Vdss (L/kg)2.42.2
t1/2 (ng/mL)54
Cmax (ng/mL)38102193
tmax (h)1.04.0
AUC0-inf (ng/mL·h)2304623807
F (%)110106
Animal Model:Female NSG mice (implanted subcutaneously with 2 × 106 MOLM-13 tumor cells)
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
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.
体外研究：
DHODH-IN-22 (compound 29) exhibits antiproliferative activity against MOLM-13 and THP-1 cells.
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