BAY-2402234 是一种选择性二氢乳清酸脱氢酶的抑制剂,可研究骨髓恶性肿瘤。
半岛bd体育手机客户端 描述
BAY-2402234 is an inhibitor of dihydroorotate dehydrogenase (DHODH) for the treatment of myeloid malignancies.BAY 2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity.
体外活性
BAY-2402234 induces differentiation of AML cell lines also in a sub-nanomolar to low-nanomolar range which demonstrates the anticipated mode of action in cellular mechanistic assays[1]. BAY-2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity. It potently inhibits proliferation of AML cell lines in the sub-nanomolar to low-nanomolar range in vitro.
体内活性
BAY-2402234 exhibits strong in vivo anti-tumor efficacy in monotherapy in several subcutaneous and disseminated AML xenografts and AML patient-derived xenograft (PDX) models. BAY-2402234 induces AML differentiation in vivo as detected by upregulation of differentiation cell surface markers in xenograft and PDX models after treatment with the inhibitor. Target engagement of the novel DHODH inhibitor BAY-2402234 can be observed by increase of tumoral and plasma dihydroorotate levels after treatment with the inhibitor. Moreover, differentiation-associated transcriptomic changes are evident following a single administration of BAY-2402234 in vivo[1].
Cas No.
2225819-06-5
分子式
C21H18ClF5N4O4
分子量
520.84
储存和溶解度
DMSO:124 mg/mL(238.08 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years