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Niraparib tosylate hydrate

  Cat. No.:  DC32395   Featured
Chemical Structure
1613220-15-7
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Field of application
Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1613220-15-7
Chemical Name: Niraparib tosylate hydrate
Synonyms: Niraparib Tosylate;MK-4827, Niraparib TsOH salt hydrate;Niraparib tosylate monohydrate;Niraparib tosylate hydrate;195Q483UZD;(S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide 4-methylbenzenesulfonate hydrate;Q27252075;(S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide 4-methylbenzenesulfonate hydrate (1:1:1);2H-Indazole-7-carboxamide, 2-(4-(3S)-3-piperidinylphenyl)-, 4-methylbenzenesulfonate, hydrate (1:1:1);Zejula
SMILES: S(C1C=CC(C)=CC=1)(=O)(=O)O.O.C1(C(N)=O)=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C12
Formula: C26H30N4O5S
M.Wt: 510.6052
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
Target: PARP-2:2.1 nM (IC50) PARP-1:3.8 nM (IC50) V-PARP:330 nM (IC50) TANK-1:570 nM (IC50) PARP-3:1300 nM (IC50)
In Vivo: Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1]. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily.
In Vitro: Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1]. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) 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.
References: [1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85. [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86. [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20. [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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