JNJ-64619178 是一种选择性的、口服活性的、假不可逆的蛋白质精氨酸甲基转移酶 5 抑制剂,IC50为 0.14 nM,有用于肺癌的研究潜力。
产品描述
JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer.
体外活性
JNJ-64619178 displays effective and broad inhibition of cellular growth. JNJ-64619178 binds simultaneously to the S-adenosylmethionine (SAM)- and protein substrate- binding pockets of the PRMT5/MEP50 complex with a pseudo-irreversible mode-of-action [1].
体内活性
In several non-small cell lung cancer and small cell lung cancer mouse xenograft models, JNJ-64619178 (p.o.) causes efficient inhibition of dimethylation of SMD1/3 proteins, components of the splicing machinery and direct substrates of the methylosome [1].
Cas No.
2086772-26-9
分子式
C22H23BrN6O2
分子量
483.36
储存和溶解度
DMSO:120 mg/mL (248.26 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years