2416131-46-7
2416131-46-7 structure
- Name: NX-2127
- Chemical Name: NX-2127
- CAS Number: 2416131-46-7
- Molecular Formula: C39H45N9O5
- Molecular Weight: 719.83
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
- Create Date: 2023-06-18 16:12:49
- Modify Date: 2025-08-22 16:14:52
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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].
| Name | NX-2127 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| In Vitro | 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]。 |
| References |
| Molecular Formula | C39H45N9O5 |
|---|---|
| Molecular Weight | 719.83 |