ML264 是抗肿瘤剂,能够特异性地抑制 Krüppel 样因子 5 表达。
产品描述
ML264 is a selective kruppel-like factor 5 (KLF5) inhibitor, which potently Inhibits growth of Colorectal Cancer.
体外活性
ML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. ML264 has significant effects at submicromolar doses on other cell types as well, including HCT116 (human colorectal carcinoma), HT29 (human colorectal adenocarcinoma), and SW620 (human colorectal adenocarcinoma). The IEC-6 anti-target (a nontransformed rat intestinal epithelial cell line) is largely unaffected, with inhibition below 50% at the highest dose[1].This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile[2].
体内活性
In an established xenograft mouse model of colon cancer, ML264 efficiently inhibits growth of the tumor within five days of treatment. this effect is caused by a significant reduction in proliferation and that ML264 potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5[2].
细胞实验
For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10μM ML264 or with vehicle (DMSO). Live cells are collected at 24, 48 and 72 hours post treatment and their numbers are determined by counting using a Coulter counter; In MTS assay, DLD-1 and HCT116 cells are treated with 10μM ML264 or with vehicle (DMSO). After 24, 48, and 72 hours of incubations, 20 μL of MTS solution is added to each well and an analysis is performed according to the manufacturer's protocol. (Only for Reference)
Cas No.
1550008-55-3
分子式
C17H21ClN2O4S
分子量
384.88
别名
CID-51003603
储存和溶解度
Ethanol:<1 mgml
DMSO:71 mg/mL (184.5 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years