Cas No.: | 1449746-00-2 |
Chemical Name: | 5-fluoro-2-(4-((methylamino)methyl)phenyl)benzofuran-7-carboxamide hydrochloride |
Synonyms: | CVL218,CVL-218,CVL 218 |
SMILES: | O=C(C1=C(OC(C2=CC=C(CNC)C=C2)=C3)C3=CC(F)=C1)N.[H]Cl |
Formula: | C17H16ClFN2O2 |
M.Wt: | 334.775 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [1]. He JX, et al. Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution. Oncotarget. 2017 Jan 17;8(3):4156-4168. [2]. Nie D, et al. Cancer-Cell-Membrane-Coated Nanoparticles with a Yolk-Shell Structure Augment Cancer Chemotherapy. Nano Lett. 2020 Feb 12;20(2):936-946. |
Description: | Mefuparib hydrochloride is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively; displays >406-fold over other major nuclear PARPs including PARP3, TNKS1, TNKS2 and PARP6; reduces poly(ADP-ribose) formation, enhances γH2AX levels, induces G2/M arrest and subsequent apoptosis in homologous recombination repair (HR)-deficient cells; 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. |
References: | References 1. He JX, et al. Oncotarget. 2017 Jan 17;8(3):4156-4168. View Related Products by Target PARP |