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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-KSQ-4279
KSQ-4279

Chemical Structure : KSQ-4279

CAS No.: 2446480-97-1

KSQ-4279 (KSQ4279, RO7623066)

货号: PC-73318Not For Human Use, Lab Use Only.

KSQ-4279 (RO7623066) is a potent, selective, first-in-class inhibitor of USP1, shows anti-proliferative effects in a subset of cell lines, including mutations in BRCA1/2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

KSQ-4279 (RO7623066) is a potent, selective, first-in-class inhibitor of USP1 with Ki of 1.2 nM, shows anti-proliferative effects in a subset of cell lines, including mutations in BRCA1/2.
KSQ-4279 has a unique mode of allosteric binding to USP1 and a high degree of selectivity over other family members.
USP1 is a protein regulating DNA damage response (DDR).
KSQ-4279 demonstrated efficacy both as a single agent and in combination with PARP inhibitors across multiple BRCA/HRD xenograft model.

物理化学性质&存储条件

分子量 534.547
分子式 C27H25F3N8O
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

6-(4-Cyclopropyl-6-methoxypyrimidin-5-yl)-1-(4-(1-isopropyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-1H-pyrazolo[3,4-d]pyrimidine

参考文献

1. Sol Shenker, et al. Cancer Res (2021) 81 (13_Supplement): 1337.

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