| Description | GDC-0339 is discovered as a potential treatment of multiple myeloma. GDC-0339 is an orally bioavailable and well-tolerated inhibitor of the pan-Pim kinase (Kis: 0.03 nM, 0.1 nM, and 0.02 nM for Pim1, Pim2, and Pim3, respectively). |
| In vitro | GDC-0339 对MM.1S细胞具有细胞静止作用，其IC50为0.1 μM。GDC-0339处理引起了一系列Pim下游信号传导事件，这与Pim激酶的抑制作用相一致[2]。 |
| In vivo | GDC-0339 的半衰期为 t1/2=0.9 小时。在为期 21 天的实验中，每天通过口服给予 1-300 mg/kg 的剂量，GDC-0339 对 RPMI8226 和 MM.1S 人类多发性骨髓瘤异种移植小鼠模型显示出强效活性[2]。 |
| Target activity | Pim1:0.03 nM(Ki), Pim3:0.02 nM(Ki), Pim2:0.1 nM(Ki) |
| molecular weight | 465.5 |
| Molecular formula | C20H22F3N7OS |
| CAS | 1428569-85-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (107.41 mM) |
| References | 1. Takahashi RH, et al. CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339. Drug Metab Dispos. 2017 Oct;45(10):1084-1092. 2. Wang X, et al. Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. J Med Chem. 2019 Feb 28;62(4):2140-2153. |