l General Information |
Product Name | Niraparib (MK-4827) |
General description | Niraparib is an orally bioavailable inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2 (PARP-1 and -2), with antineoplastic activity. |
Synonym | 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide |
Purity | ≥98.0%(HPLC) | CAS Number | 1038915-60-4 |
Formula | C19H20N4O | Molecular Weight | 320.39 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | solid |
Solubility(25℃) | DMSO | ≥50mg/mL |
Ethanol | ≥50mg/mL |
Water | Insoluble |
l Biological Information |
Biochem/Physiol
Actions | Niraparib is an orally bioavailable inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2 (PARP-1 and -2), with antineoplastic activity. Upon administration, niraparib binds to and inhibits the activity of PARP-1 and -2, thereby inhibiting PARP-1 and -2-mediated DNA repair, enhancing the accumulation of DNA strand breaks, promoting genomic instability and resulting in apoptosis. The PARP family of proteins catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks. Niraparib is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. |
Application | Niraparib is a small molecule inhibitor of poly ADP-ribose polymerase that is used in the therapy of selected patients with refractory and advanced ovarian carcinoma. Niraparib therapy is associated with a low rate of transient elevations in serum aminotransferase during therapy, but has not been ed to instances of clinically apparent liver injury. |
l Storage |
Storage temp. | -20℃ |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
