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DHODH-IN-22
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DHODH-IN-22图片
CAS NO:2450341-75-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
DHODH-IN-22 是一种有效且具有选择性和口服活性的二氢乳清酸脱氢酶 (DHODH) 抑制剂,IC50为 0.3 nM。DHODH-IN-22可用于研究急性髓系白血病 (AML)。
生物活性

DHODH-IN-22 is a potent, selective and orally activedihydroorotate dehydrogenase(DHODH)inhibitor with anIC50value 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]

体外研究
(In Vitro)

DHODH-IN-22 (compound 29) exhibits antiproliferative activity against MOLM-13 and THP-1 cells[1].

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.
体内研究
(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)7.37.6
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 × 106MOLM-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.
分子量

548.88

Formula

C21H21ClF4N6O5

CAS 号

2450341-75-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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