Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
Molecular Weight | 356.85 |
CAS Number | 1038915-64-8 |
Solubility (25°C) | DMSO 150 mg/mL Water 90 mg/mL |
Storage | 2-8°C, dry, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Dea Slade. Genes Dev. PARP and PARG inhibitors in cancer treatment
Related PARP Products |
---|
DSB-1522
DSB-1522 is a PARP1 inhibitor that can be used in tumor-related studies. |
DM-5167
DM-5167 is a PARP1 inhibitor that can be used in studies related to triple negative breast cancer. |
NMS-03305293
NMS-03305293 is a PARP inhibitor with high selectivity for PARP1 isoforms and low DNA capture effect, which specifically kills BRCA mutated tumor cells. In addition, NMS-03305293 can penetrate the blood-brain barrier and can be used in studies related to CNS tumors and brain metastatic tumors. |
SNV1521
SNV1521 is a potential best-in-class (BIC), highly selective and CNS-permeable PARP1 inhibitor. |
Basroparib
Basroparib is an orally active selective inhibitor of end-anchor polymerase (TNKS) and an inhibitor of ribose polymerase (PARP) with antitumor activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.