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首页-抗体药物偶连体和PROTACs-PROTAC-NX-2127
NX-2127

Chemical Structure : NX-2127

CAS No.: 2416131-46-7

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NX-2127 (NX2127)

货号: PC-20560Not For Human Use, Lab Use Only.

NX-2127 (NX2127) is a hetero-bifunctional, orally active PROTAC that induces the degradation of BTK and IKZF3 ubiquitination and proteasomal degradation in cells through recruitment of cereblon (CRBN).

规格 价格 库存 数量
5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NX-2127 (NX2127) is a hetero-bifunctional, orally active PROTAC that induces the degradation of BTK and IKZF3 ubiquitination and proteasomal degradation in cells through recruitment of cereblon (CRBN).
NX-2127 degrades BTK in multiple B cell lymphoma lines with DC50 values in the range of 1-13 nM.
NX-2127 displays efficient cellular degradation yet binds to WT and mutant BTK with affinities that render covalent and noncovalent BTK inhibitors ineffective.
NX-2127 drives cellular ternary complex formation between BTK and CRBN by inducing positive cooperativity in both WT and acquired resistance mutant settings.
NX-2127 induces potent degradation of C481S, T474I, V416L, and L528W-mutant BTK and suppresses activation marker expression on cells harboring these mutations.
NX-2127 demonstrates oral bioavailability across pre-clinical species and shows robust tumor growth inhibition in WT and mutant mouse models of lymphoma upon once daily PO dosing.

物理化学性质&存储条件

分子量 719.85
分子式 C39H45N9O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-

参考文献

1. Jeffrey T. Mihalic, et al. Cancer Res (2023) 83 (7_Supplement): 3423.

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