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DHODH-IN-21
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-21图片
CAS NO:2450341-39-4
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-21 (compound 19) 是一种具有口服活性的选择性二氢乳酸脱氢酶 (DHODH) 抑制剂,其IC50值为 1.1 nM。DHODH-IN-21 具有抗癌活性,可用于急性髓性白血病 (AML) 的研究。
生物活性

DHODH-IN-21 (compound 19) is an orally active selectivedihydroorotate dehydrogenase(DHODH) inhibitor with anIC50value 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)

体外研究
(In Vitro)

DHODH-IN-21 (compound 19) inhibits the proliferation of MOLM-13 and THP-1 cells with the IC50values of 2.0 nM and 5.0 nM, respectively[1].

体内研究
(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].

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)
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(hong/mL)16,0669214
F%103167
分子量

518.85

Formula

C20H19ClF4N6O4

CAS 号

2450341-39-4

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.