NX-2127

NX-2127

N646876-5mg

5mg

≥98%

避光,-80℃储存

超低温冰袋运输

NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTK C481S in cells. NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib . 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. In Vitro NX-2127 inhibits proliferation of BTK-C481S mutant TMD8 cells with an EC 50 value In Vivo NX-2127 (1 mg/kg; po; once daily for 14 days) demonstrates potent degradation of BTK in cynomolgus monkeys in vivo . NX-2127 (po) leads to dose-proportional exposure in plasma and BTK degradation to Form:Solid

NX-2127 是一种口服强效 BTK 抑制剂，能诱导细胞中突变的 BTK C481S 降解。与伊布替尼（HY-10997）相比，NX-2127 能更有效地抑制 BTK C481S 突变体 TMD8 细胞的增殖。NX-2127 可催化 Ikaros 的降解。

2416131-46-7

C39H45N9O5

719.83 g/mol

O=C1C2=CC(N3C[C@H](CN4CCC(C5=CC=C(C=C5)NC6=C(N=CC(N7CCCCC7)=N6)C(N)=O)CC4)CC3)=CC=C2C(N1C8C(NC(CC8)=O)=O)=O

DMSO : 100 mg/mL (138.92 mM; Need ultrasonic)