Niraparib hydrochloride NEW
Price | $34 | $55 | $80 |
Package | 2mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: Niraparib hydrochloride | CAS No.: 1038915-64-8 |
Purity: 99.26% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | Niraparib hydrochloride |
Description | Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway. |
In vitro | MK-4827 significantly enhances the effectiveness of radiation on human tumor xenografts (whether p53 wild-type or p53 mutant), demonstrating good tolerability in vivo. When used alone, it also exhibits efficacy against BRCA-1 deficient xenograft models. |
In vivo | In cell assays, MK-4827 exhibits inhibitory effects on PARP activity (EC50: 4 nM) and suppresses the proliferation of cancer cells carrying BRCA-1/2 mutations (IC50: 10-100 nM). It effectively inhibits PARP-1/2 (IC50: 3.8/2.1 nM) but shows significantly lower selectivity (over 100-fold) against PARP-3, V-PARP, and tankyrase-1 (IC50: 1300/330/570 nM). In MDA-MB-436 human breast adenocarcinoma cells with a BRCA-1 mutation, MK-4827 has a CC50 of 18 nM; in CAPAN-1 human pancreatic cancer cells with a BRCA-2 deficiency, the CC50 is 90 nM. Normal human prostatic and breast epithelial cells exhibit resistance to MK-4827. This indicates that PARP inhibitors like MK-4827 have selective cytotoxicity in cancer cells with BRCA-1/2 mutations, minimizing the impact on surrounding tissue. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 50 mg/mL (140.11 mM) |
Keywords | MK4827 Hydrochloride | DNA | cancer | lung | Niraparib | anti-tumor | Inhibitor | Niraparib hydrochloride | orally | damage | bioavailable | MK-4827 | Niraparib Hydrochloride | Apoptosis | MK 4827 | PARP | MK4827 | poly ADP ribose polymerase | MK 4827 Hydrochloride | MK-4827 Hydrochloride | ovarian | inhibit | breast |
Inhibitors Related | Stavudine | Sodium 4-phenylbutyrate | Tributyrin |
Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | Targeted Therapy Drug Library | FDA-Approved Drug Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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