| Bioactivity | NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTKC481S in cells. NX-2127 inhibits proliferation of BTKC481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells[1][2]. |
| Invitro | NX-2127 抑制 BTK-C481S 突变型 TMD8 细胞的增殖，EC50 值<30 nM[1]。NX-2127 增加原代人 T 细胞中 IL-2 的产生[1]。 |
| In Vivo | NX-2127（1 mg/kg；口服；每天一次，持续 14 天）在食蟹猴体内显示出 BTK 的有效降解[1]。NX-2127（口服）导致血浆中的剂量比例暴露和 BTK 降解至低于循环和脾脏 B 细胞基线水平的 10%[1]。NX-2127 在小鼠的 WT TMD8 和 C481S 突变体异种移植模型中产生优异的肿瘤生长抑制 (TGI)[1]。 |
| Name | NX-2127 |
| CAS | 2416131-46-7 |
| Formula | C39H45N9O5 |
| Molar Mass | 719.83 |
| 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]. Robbins D W, et al. Nx-2127, a degrader of BTK and IMiD neosubstrates, for the treatment of B-cell malignancies. Blood, 2020, 136: 34. [2]. Mato A, et al. A first-in-human phase 1 trial of NX-2127, a first-in-class oral BTK degrader with IMiD-like activity, in patients with relapsed and refractory B-cell malignancies. 2022. |