Description | BGB-8035 is an orally available, selective and potent BTK inhibitor with antitumor activity that inhibits BTK, TEC and EGFR.BGB-8035 is used in the study of tumors and autoimmune diseases. |
In vivo | 在 9 周龄的雌性 NOD/SCID 小鼠中,这些小鼠带有 REC-1 MCL 异种移植瘤,BGB-8035(剂量分别为 7.5、15、30 mg/kg;口服给药;每日两次)显示出剂量依赖性的抗肿瘤活性,对应的肿瘤生长抑制(TGI)值分别为 64.1%、73.6% 和 79.9%[1]。 |
Target activity | EGFR:621 nM, TEC:99 nM, BTK:1.1 nM |
Synonyms | BGB8035, BGB 8035 |
molecular weight | 453.53 |
Molecular formula | C24H31N5O4 |
CAS | 2283349-24-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
References | 1. Yunhang Guo, et al. Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases. J Med Chem. 2023 Mar 23;66(6):4025-4044. |