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: 2024-01-10 14:01:30
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	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
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	[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.

Molecular Formula	C₃₉H₄₅N₉O₅
Molecular Weight	719.83