| Bioactivity | BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research[1]. |
| Target | IC50: 1.1 nM (BTK), 99 nM (TEC), and 621 nM (EGFR) |
| Invitro | BGB-8035 对 HEK293 和 Ramos 细胞基本无毒 (IC50>10 μM)[1]。 |
| In Vivo | BGB-8035 (7.5, 15, 30 mg/kg; 灌胃给药; 每天两次; 16 天) 表现出剂量依赖性抗肿瘤活性[1]。 BGB-8035 (1, 3, 10, 30 mg/kg; 灌胃给药; 每天两次; 13 天) 在 8-9 周大的 Lewis 大鼠CIA 模型中以剂量依赖的方式抑制关节炎，并防止 CIA 模型相关的体重减轻[1]。 Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs[1]. |
| Name | BGB-8035 |
| CAS | 2283349-24-4 |
| Formula | C24H31N5O4 |
| Molar Mass | 453.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
BGB-8035
CAS: 2283349-24-4 F: C24H31N5O4 W: 453.53
BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.