DHODH-IN-21

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DHODH-IN-21

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CAS NO:

2450341-39-4

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)

Parameter	Mouse	Rat
CL (mL/min/kg)	11	32
V_dss(L/kg)	1.3	2.3
t_1/2(h)	2.3	2.0
C_max(ng/mL)	4047	1713
t_max(h)	0.42	1.7
AUC_0→inf(hong/mL)	16,066	9214
F%	103	167

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.