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NX-2127

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Chemical Structure| 2416131-46-7 同义名 : -
CAS号 : 2416131-46-7
货号 : A2020200
分子式 : C39H45N9O5
纯度 : 98%
分子量 : 719.832
MDL号 : MFCD34789579
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(145.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 NX-2127 is characterized as a potent oral BTK inhibitor that facilitates the degradation of the BTKC481S mutation in cells and is more effective than Ibrutinib in halting the proliferation of BTKC481S mutant TMD8 cells. It also promotes the breakdown of Ikaros (IKZF1) and Aiolos (IKZF3), with IC50 values of 25 nM and 54 nM, respectively. Furthermore, NX-2127 activates T cells and elevates IL-2 production in primary human T cells[1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.95mL

1.39mL

0.69mL

13.89mL

2.78mL

1.39mL
参考文献

[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.