GDC-0853 (GDC-0853) 是一种有效的、选择性的、口服的、非共价的 bruton's 酪氨酸激酶 (Btk) 抑制剂，对 WT Btk 和 C481S 的 Kis 分别为 0.91 nM、1.6、1.3、12.6 和 3.4 nM 、C481R、T474I、T474M 突变体。 GDC-0853 具有用于类风湿性关节炎和系统性红斑狼疮研究的潜力。
| Cas No. | 1434048-34-6 |
| 别名 | GDC-0853 |
| Canonical SMILES | O=C1C(NC(C=C2)=NC=C2N3CCN(C4COC4)C[C@@H]3C)=CC(C5=CC=NC(N6C(C7=CC(CC(C)(C)C8)=C8N7CC6)=O)=C5CO)=CN1C |
| 分子式 | C37H44N8O4 |
| 分子量 | 664.8 |
| 溶解度 | DMSO : ≥ 23 mg/mL (34.60 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Fenebrutinib (GDC-0853) is a potent, selective, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with a Ki of 0.91 nM. References:
[1]. Erickson RI , et al. Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats. J Pharmacol Exp Ther. 2017 Jan;360(1):226-238. |
