ZLD1039 是一种口服有效的、高选择性 EZH2 抑制剂。ZLD1039 高效抑制 EZH2 野生型及 Y641F 和 A677G 突变型，IC50 分别为 5.6、15 和 4.0?nM。ZLD1039 抑制乳腺肿瘤的生长和转移。
产品描述
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
体外活性
ZLD1039 inhibited the H3K27me3 and H3K27me2 levels in MCF-7 (0.25~2 μM, 4 days) and MDA-MB-231 (1~4 μM, 4 days) cells in a dose-dependent manner[1].
Cas No.
1826865-46-6
分子式
C36H48N6O3
分子量
612.8
别名
ZLD-1039;ZLD 1039
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
