| Description | Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine renal-type glutaminase (KGA) variant inhibitor, showed antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model. |
| In vitro | Glutaminase-IN-1（CPD20）是CB839的衍生物，作为肾型谷氨酰胺酶（KGA）的构象抑制剂，其IC50为1 nM。Glutaminase-IN-1展现了优于CB839的细胞摄取能力和抗肿瘤活性。在A549、H2、Caki-1、和HCT116细胞系中，Glutaminase-IN-1的IC50分别为17 nM、6.78 μM、19 nM和9 nM。相较于相应的BPTES及CB839[1]，Glutaminase-IN-1展示了更卓越的KGA抑制活性。 |
| In vivo | Glutaminase-IN-1（10 mg/kg，皮下注射）显著减少了HCT116肿瘤的大小和重量，与CPD20相比肿瘤重量显著降低40%。此外，Glutaminase-IN-1还显著延长了携带H22[1]的小鼠的生存时间。 |
| Target activity | A549 cells:17 nM, KGA:1 nM, HCT116 cells:9 nM, Caki-1 cells:19 nM, H2:6.78 μM |
| Synonyms | CB839 derivative |
| molecular weight | 618.47 |
| Molecular formula | C26H24F3N7O3Se |
| CAS | 2247127-79-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (161.69 mM), Sonication is recommended. H2O: 1 mg/mL (1.61 mM), Sonication is recommended. |
| References | 1. Chen Z, et al. Novel 1,3,4-Selenadiazole Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity. J Med Chem. 2018 Dec 13. |