| Bioactivity | KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice[1][2]. |
| Invitro | KIN-8194 (0-1 μM，7 天) 抑制 MCL 细胞系 (Maver-1、JeKo-1、Mino、Rec-1 和 Granta-519) 和原代细胞的生长[1].KIN-8194 (0-1 μM，7 天) 通过抑制 HCK 减少 MCL 细胞系增殖[1]。KIN-8194 (100 nM，6 h) 以 HCK 依赖性方式抑制 Maver-1 和 Granta-519 细胞中的 AKT-S6 信号通路[1]。KIN-8194 (0-1 μM，30 min) 以 HCK 依赖性方式抑制 MCL 细胞 (JeKo-1 和 Granta-519) 与纤连蛋白或基质细胞的粘附[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> KIN-8194 相关抗体: |
| In Vivo | KIN-8194 (12.5-50 mg/kg，口服，一次) 在 MYD88 突变的 TMD-8 ABC DLBCL 异种移植小鼠模型中以剂量依赖性方式阻断 pHCK 和 pBTK[2]。KIN-8194 (50 mg/kg，口服，每日，6 周) 可抑制 MYD88 突变 TMD-8 ABC DLBCL 异种移植小鼠模型中的肿瘤生长[2]。KIN-8194 (30 mg/kg，口服，每日，22 天) 联合 Venetoclax (HY-15531) 延长 ibrutinib 耐药 BTKCys481Ser TMD-8 细胞异种移植小鼠的中位生存时间[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 330786-01-1 |
| Formula | C28H33N7O |
| Molar Mass | 483.61 |
| 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]. Lantermans HC, et al. The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma. Leukemia. 2024 Mar 7. [2]. Yang G, et al. The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. Blood. 2021 Nov 18;138(20):1966-1979. |