Mefuparib|CVL218|CAS 1449746-00-2|COVID-19

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

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC33651	ML188	ML188 is a Potent Noncovalent Small Molecule Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) 3CL Protease. The X-ray structure of SARS-CoV 3CLpro bound with ML188 was instrumental in guiding subsequent rounds of chemistry optimiz
DC10662	GC-376	GC376 is a novel, first-in-class, small molecule protease inhibitor with a favorable therapeutic index demonstrated in preclinical studies. A common feature of viruses in the picornavirus-like supercluster (including coronaviruses) is a 3C or 3C-like prot
DC20446	Mefuparib hydrochloride(CVL218)	Mefuparib(CVL218) hydrochloride is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively.CVL218 was more potent than Remdesivir in blocking Coronavirus infection of cells and equally as potent as Remdesivir in blocking replication of virus once it has entered the cells.
DC11407	Asapiprant(BGE-175)	Asapiprant (BGE-175) is a potent and specific antagonist of human PGD2/PTGDR signaling with Ki of 0.44 nM. BGE-175 is currently in a Phase 2 clinical trial to test whether it can prevent disease progression and mortality in older patients hospitalized wit
DC23957	RO-9187	A potent HCV NS5B RNA polymerase inhibitor.
DC22771	Proxalutamide	Proxalutamide (GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) for the potential treatment of COVID-19, prostate cancer, and breast cancer.

Mefuparib hydrochloride(CVL218)