ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >MK-4827 (tosylate)

MK-4827 (tosylate)

MK-4827 (tosylate) Structure
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

MK-4827 (tosylate) Properties

Melting point >142oC (dec.)
storage temp. -20°C Freezer
solubility Methanol (Slightly)
form Solid
color Off-White to Pale Yellow
InChIKey LCPFHXWLJMNKNC-XOIICWPPNA-N
SMILES S(C1C=CC(C)=CC=1)(O)(=O)=O.C(C1=CC=CC2=CN(C3C=CC([C@H]4CNCCC4)=CC=3)N=C12)(=O)N |&1:23,r|

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

Global( 131)Suppliers
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

MK-4827 (tosylate) Spectrum

Niraparib TsOH niraparib p-toluenesulfonate MK-4827(Niraparib) tosylate MK-4827 (tosylate) (3S)-3-[4-[7-(Aminocarbonyl)-2H-indazol-2-yl]phenyl]piperidine tosylate MK-4827, Niraparib TsOH salt Niraparib(MK-4827) tosylate NIRAPARIB TOSYLATE;MK 4827 TOSYLATE;MK4827 TOSYLATE 2H-Indazole-7-carboxamide,2-[4-[(3S)-3-piperidinyl]phenyl]-,4-methylbenzenesulfonate(1:1) Niraparib TOS MK-4827 (tosylate) ISO 9001:2015 REACH Niraparib Tosylate (MK-4827) Niraparib Tosylate (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide 4-methylbenzenesulfonate Niraparib tosylate monohydrate (S)-2-(4-(piperidin-3-yl)phenyl)-2H-isoindole-4-carboxamide compound with 1-methyl-4-(methylsulfonyl)benzene (1:1) hydrate Niraparib Tosilate 1038915-73-9 C19H20N4OC7H8O3S