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首页-抗体药物偶连体和PROTACs-PROTAC-IKZF2 degrader 25
IKZF2 degrader 25

Chemical Structure : IKZF2 degrader 25

CAS No.:

IKZF2 degrader 25

货号: PC-26522Not For Human Use, Lab Use Only.

IKZF2 degrader 25 is a potent, highly selective, and orally efficacious IKZF2 degrader with DC50 of 1.78 nM (Dmax = 93.2%, HEK293T cells), with minimal IKZF1/3 degradation.

规格 价格 库存 数量
25 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IKZF2 degrader 25 is a potent, highly selective, and orally efficacious IKZF2 degrader with DC50 of 1.78 nM (Dmax = 93.2%, HEK293T cells), with minimal IKZF1/3 degradation.
IKZF2 degrader 25 potently degraded endogenous IKZF2 in Jurkat cells with a DC50 of 1.59 nM and Dmax of 92.2%, demonstrating markedly higher potency than DKY709 (DC50 = 9.56 nM, Dmax = 80.5%) and pomalidomide (DC50 > 10,000 nM, Dmax = 40.7%).
IKZF2 degrader 25 elicited dose-dependent decreases of endogenous IKZF2 and near-complete degradation was achieved by compound 25 (100 nM) at 24 h in Jurkat cells.
IKZF2 degrader 25 shows minimal degradation effects on IKZF1, IKZF3, SALL4, GSPT1, CK1α and ZFP91.
IKZF2 degrader 25 promotes the formation of a stable ternary complex between IKZF2 and CRBN to drives its robust degradation. exhibited IKZF2 degradation activity via a Cullin-CRBN dependent pathway.
IKZF2 degrader 25 increased interferon-γ (IFNγ) production in exhausted CD4+ and CD8+ effector T cells (Teffs), modulated the phenotype and function of Treg cells, thereby enhancing antitumor T cell-mediated immunity.
IKZF2 degrader 25 significantly suppressed tumor growth and showed synergistic anticancer efficacy with anti-PD-1 therapies, in B16F cell xenograft tumor model.

物理化学性质&存储条件

分子量 577.69
分子式 C33H35N7O3
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

3-(4-(4-(((2-(2,6-Dioxopiperidin-3-yl)-3-methyl-1-oxo-1,2,3,4-tetrahydrophthalazin-6-yl)amino)methyl)benzyl)piperazin-1-yl)benzonitrile

参考文献

1. Wang Y, et al. J Med Chem. 2026 Apr 7. doi: 10.1021/acs.jmedchem.6c00500.

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