| Description | BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth. |
| In vitro | 50 mg/kg,i.p. BQU57在负荷人肺H2122肿瘤的小鼠体内,明显抑制RalA和RalB的活化,并且剂量依赖性抑制肿瘤生长. |
| In vivo | BQU57抑制H2122和H358细胞系中RalA与RalB活化,从而引起细胞生长抑制。 |
| Cell experiments | Growth inhibition on human lung cancer cells by the compounds are measured under anchorage-independent conditions in soft agar. Cells are seeded into 6-well plates (coated with a base layer made of 2.0 mL of 1% low-melting-point agarose) at 15,000 cells per well in 3.0 mL of 0.4% low-melting-point agarose containing various concentration of drug. Two to four weeks (depending on cell line) after incubation, cells are stained with 1.0 mg/mL Nitro Blue Tetrazolium and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in 50% reduction in colony number compared to DMSO treated control. After 48 hr, cells are subjected to the soft agar colony formation assay. (Only for Reference) |
| molecular weight | 334.3 |
| Molecular formula | C16H13F3N4O |
| CAS | 1637739-82-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 16 mg/mL (47.9 mM) DMSO: 40 mg/mL (119.65 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Yan C, et al. Nature. 2014, 515(7527), 443-447. |