niraparib p-toluenesulfonate
MK-4827 (tosylate)
CAS: 1038915-73-9
Molecular Formula: C26H28N4O4S
niraparib p-toluenesulfonate - Names and Identifiers
niraparib p-toluenesulfonate - Physico-chemical Properties
| Molecular Formula | C26H28N4O4S |
| Molar Mass | 492.58992 |
| Melting Point | >142oC (dec.) |
| Solubility | DMSO: ≥ 490 mg/mL |
| Appearance | Solid |
| Color | Off-White to Pale Yellow |
| Storage Condition | -20°C Freezer |
| Physical and Chemical Properties | Bioactive Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM and 2.1 nM respectively. Niraparib can increase the formation of PARP-DNA complex and lead to DNA damage, apoptosis and cell death. |
| Use | Application (3S)-3-[4-[7-(aminocarbonyl)-2H-indazol-2-yl] phenyl] piperidine p-toluene sulfonate is a pharmaceutical intermediate for the synthesis of nirapani bulk drugs, which can be used in laboratory research and development processes and chemical and pharmaceutical synthesis processes. |
| In vitro study | The micromolar concentration of niraparib sensitizes tumor cells from lung cancer, breast cancer, and prostate cancer to radiation (independent of their p53 status) but not to cells from normal tissue. Niraparib also sensitizes tumor cells to hydrogen peroxide and converts hydrogen peroxide-induced single-strand breaks to double-strand breaks upon DNA replication. |
| In vivo study | MK-4827 can enhance the effect of radiation on a variety of human tumor xenografts, whether in p53 wild type or p53 mutant. MK-4827 reduced PAR levels in tumors at 1 hour post-dose and sustained the effect for 24 hours. MK-4827 in vivo administration can prolong the life of animals after radiation treatment. MK-4827 in combination with radiotherapy significantly increased the levels of cleaved caspase-3 and γ-H2AX in the tumor. |
niraparib p-toluenesulfonate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.03 ml | 10.15 ml | 20.301 ml |
| 5 mM | 0.406 ml | 2.03 ml | 4.06 ml |
| 10 mM | 0.203 ml | 1.015 ml | 2.03 ml |
| 5 mM | 0.041 ml | 0.203 ml | 0.406 ml |
Last Update：2024-01-02 23:10:35
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Product Name: MK-4827 (tosylate) Visit Supplier Webpage Request for quotationCAS: 1038915-73-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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