Bioactivity | JDB175 is a highly selective BTK inhibitor with oral activity and excellent blood-brain barrier penetration. JDB175 shows good activity in the mouse model of central nervous system lymphoma without obvious signs of toxicity, effectively inhibits the proliferation of BTK signaling pathway of human lymphoma cells, induces cell cycle arrest, and promotes cell apoptosis [1]. |
Invitro | DB175 (15-40 μM, 48 h) 在 Namalwa, Raji 细胞中能有效抑制 BTK 的磷酸化,下调 cyclin D1 和CDK2 的表达,上调 P21 的表达[1]。JDB175 (0-60 μM, 48 h, 72 h) 在Namalwa, SU-DHL-4, Raji, Ramos, TMD-8 细胞中对细胞活力有时间和剂量依赖性的抑制作用[1]。JDB175 (15 μM, 48 h) 在 Namalwa, SU-DHL-4, Raji, Ramos 细胞中显著增加了 G0/G1 期分布[1]。JDB175 (20-40 μM, 72 h) 在 Namalwa, SU-DHL-4, Raji, Ramos 细胞中显示出较强的诱导凋亡作用[1]。 0 --> JDB175 相关抗体: Cell Viability Assay[1] Cell Line: |
In Vivo | JDB175 (10 mg/kg, 口服, 0.5 h) 在大鼠中具有穿透血脑屏障的强大潜力,在抑制中枢神经系统淋巴瘤方面表现出良好的能力[1]。JDB175 (150 mg/kg, 口服, 3 天) 在裸鼠中枢神经系统淋巴瘤肿瘤模型中对肿瘤表现出有效的抑制作用和良好的安全性[1]。 Animal Model: |
Name | JDB175 |
CAS | 2635328-79-7 |
Formula | C26H21F3N4O2 |
Molar Mass | 478.47 |
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]. Xia Y, et al. A novel Bruton's tyrosine kinase inhibitor JDB175 shows potent efficacy to suppress central nervous system lymphoma. MedComm (2020). 2023 Nov 4;4(6):e424. |