Serdemetan 是一种HDM2泛素连接酶拮抗剂,能诱导p53野生型细胞的早期凋亡。
产品描述
Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
体外活性
在实体移植瘤和ALL移植瘤种,口服 JNJ-26854165(20 mg/kg)能够使EFS分布显现显著差异.
体内活性
在白血病细胞系中,JNJ-26854165能够抑制细胞生长,并且诱导细胞凋亡,对于OCI-AML-3(IC50=0.24 μM), MOLM-13(IC50=0.33 μM),NALM-6(IC50=0.32 μM)和REH(IC50=0.44 μM)均有抑制作用。在人类癌细胞系中(H460,A549,p53-WT-HCT116,和p53-null-HCT116),JNJ-26854165能够抑制细胞增殖。
细胞实验
Cell lines are maintained in RPMI 1640 medium containing 10% heat-inactivated fetal calf serum (FCS). OCI-AML-3, MOLM-13, NB4 and U937 cells are derived from acute myelogenous leukemia (AML) patients, K562 from a chronic myelogenous leukemia (CML) patient in blast crisis, and NALM-6, REH, P12-ICHIK(Only for Reference)
Cas No.
881202-45-5
分子式
C21H20N4
分子量
328.42
别名
N-[2-(1H-吲哚-3-基)乙基]-N'-(4-吡啶基)-1,4-苯二胺;JNJ-26854165
储存和溶解度
DMSO:61 mg/mL (185.7 mM)
Ethanol:2 mg/mL (6.08 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years