MK-4827 (tosylate)
- CAS No.
- 1038915-73-9
- Chemical Name:
- MK-4827 (tosylate)
- Synonyms
- Niraparib Tosylate;Niraparib TOS;Niraparib TsOH;MK-4827 (tosylate);Niraparib Tosilate;Niraparib(MK-4827) tosylate;MK-4827(Niraparib) tosylate;niraparib p-toluenesulfonate;MK-4827, Niraparib TsOH salt;Niraparib Tosylate (MK-4827)
- CBNumber:
- CB52682012
- Molecular Formula:
- C26H28N4O4S
- Molecular Weight:
- 492.58992
- MOL File:
- 1038915-73-9.mol
- Modify Date:
- 2024/5/18 8:51:57
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P305+P351+P338 |
MK-4827 (tosylate) Chemical Properties,Uses,Production
Description
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively; with significant activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP, and Tank1. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis, and shows anti-tumor activity.
Uses
Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
in vitro
In a whole-cell assay, Niraparib (MK-4827) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM. Niraparib tosylate hydrate inhibits the proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. Niraparib tosylate hydrate displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole-cell assay. Niraparib tosylate hydrate inhibits PARP within 15 minutes of treatment, reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.
MK-4827 (tosylate) Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
Beijing Hope Pharmaceutical Co., Ltd. | +86-010-67886402 +8613611125266 | China | 71 | 58 | Inquiry |
Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 | China | 10978 | 58 | Inquiry |
hebei hongtan Biotechnology Co., Ltd | +86-86-1913198-3935 +8617331935328 | China | 973 | 58 | Inquiry |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29826 | 58 | Inquiry |
WinWin Chemical CO., Limited | +86-0086-577-64498589 +86-15355981851 | China | 14279 | 58 | Inquiry |
Related articles
- MK-4827 (tosylate)
- To validate that MK-4827 (Niraparib) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for....
- Aug 26,2019
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