| Description | Tenalisib (RP6530) (RP6530) is a potent and selective inhibitor of PI3Kδ and PI3Kγ(IC50 values of 25 and 33 nM, respectively.) |
| In vitro | 在HEL-RS和HEL-RR细胞中，Tenalisib表现出中等水平的增殖抑制作用（10 μM时抑制率为33-46%）。将10 μM Tenalisib与ruxolitinib联合使用，表现出协同效应，显著增强了对增殖的抑制作用（HEL-RS细胞>90%，HEL-RR细胞>70%）。在HEL-RR细胞中，先于ruxolitinib添加4小时的5 μM Tenalisib，可显著降低ruxolitinib的EC50值（至5.8 μM）。 |
| In vivo | Tenalisib 每日给药2次（每次≥200 mg）在难治疗患者中的疗效明显。 |
| Target activity | PI3Kγ:33 nM, PI3Kδ:25 nM |
| Synonyms | RP6530 |
| molecular weight | 415.42 |
| Molecular formula | C23H18FN5O2 |
| CAS | 1639417-53-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (240.72 mM) |
| References | 1. Vakkalanka S, et al. RP6530, a dual PI3K δ/γ inhibitor, potentiates ruxolitinib activity in the JAK2-V617F mutant erythroleukemia cell lines. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2704. doi:10.1158/1538-7445.AM2015-2704 2. Carmelo C, et al. A Dose Escalation Study of RP6530, a Novel Dual PI3K Delta/Gamma Inhibitor, in Patients with Relapsed/Refractory Hematologic Malignancies. Blood 2015 126:1495; |