SAR 131675 是一种选择性的VEGFR3抑制剂,其IC50=23 nM。
产品描述
SAR 131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
体外活性
KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition. [1]
Cas No.
1433953-83-3
分子式
C18H22N4O4
分子量
358.4
别名
SAR 131675
储存和溶解度
Ethanol:<1 mgml
H2O:<1 mgml
DMSO:16.67 mg/mL (46.51 mM),ultrasonic and adjust pH to 2 with HCl
Powder: -20°C for 3 years
In solvent: -80°C for 2 years