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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-Mefuparib
Mefuparib

Chemical Structure : Mefuparib

CAS No.: 1392502-82-7

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Mefuparib (CVL218, CVL-218)

货号: PC-25001Not For Human Use, Lab Use Only.

Mefuparib (CVL218) is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively.

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

生物&药学活性

Mefuparib (CVL218) is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively.
Mefuparib displays >406-fold over other major nuclear PARPs including PARP3, TNKS1, TNKS2 and PARP6.
Mefuparib reduces poly(ADP-ribose) formation, enhances γH2AX levels, induces G2/M arrest and subsequent apoptosis in homologous recombination repair (HR)-deficient cells.
Mefuparib shows potent in vitro and in vivo proliferation and growth inhibition against HR-deficient cancer cells and synergistic sensitization of HR-proficient xenografts to the anticancer drug temozolomide.

物理化学性质&存储条件

分子量 298.32
分子式 C17H15FN2O2
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

5-fluoro-2-(4-((methylamino)methyl)phenyl)benzofuran-7-carboxamide

参考文献

1. He JX, et al. Oncotarget. 2017 Jan 17;8(3):4156-4168.

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