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ChemicalBook > CAS DataBase List > Niraparib

Niraparib

Uses
Product Name
Niraparib
CAS No.
1038915-60-4
Chemical Name
Niraparib
Synonyms
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide;MK-4827 98.00%;Niraparib (MK-4827);CS-2299;iraparib;Niraparib;EOS-60867;Niraparib base;MK4827 (Niraparib);Niraparib USP/EP/BP
CBNumber
CB82514860
Molecular Formula
C19H20N4O
Formula Weight
320.39
MOL File
1038915-60-4.mol
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Niraparib Property

Melting point:
187-189°C
Boiling point:
463.6±45.0 °C(Predicted)
Density 
1.34
storage temp. 
2-8°C(protect from light)
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
15.36±0.30(Predicted)
form 
Solid
color 
Pale Yellow to Light Yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC
Product number
N481400
Product name
Niraparib
Packaging
2.5mg
Price
$450
Updated
2021/12/16
ApexBio Technology
Product number
A3617
Product name
MK-4827
Packaging
50mg
Price
$490
Updated
2021/12/16
Matrix Scientific
Product number
153552
Product name
(S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide
Purity
95%
Packaging
5mg
Price
$556
Updated
2021/12/16
ApexBio Technology
Product number
A3617
Product name
MK-4827
Packaging
100mg
Price
$740
Updated
2021/12/16
Apolloscientific
Product number
OR321439
Product name
(S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide
Purity
99%
Packaging
5g
Price
$790
Updated
2021/12/16
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Niraparib Chemical Properties,Usage,Production

Uses

Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.

Description

(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide is also known as MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 (The poly(ADP-ribose) polymerase) with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It has been recently approved by FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell death.

Uses

Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.

Definition

ChEBI: Niraparib is a 2-[4-(piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide that has S-configuration. It is a potent inhibitor of PARP1 and PARP2 (IC50 of 3.8 and 2.1 nM, respectively) and approved as a first-line maintenance treatment for women with advanced ovarian cancer after responding to platinum-based chemotherapy. It has a role as an antineoplastic agent, an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor, a radiosensitizing agent and an apoptosis inducer.

Pharmacology

The synthesis and initial pharmacology of niraparib have been published. Niraparib has affinity for PARP 1 and 2 inhibition (IC50 = 3.8 and 2.1 nM, respectively) and inhibits the proliferation of cancer cells with mutant BRCA1 and BRCA2 with IC50 values in the 10–100 nM range in vitro. Niraparib demonstrated efficacy as a single agent in a xenograft model of BRCA1-deficient cancer. Niraparib has also been reported to act as a preclinical radiosensitiser and has entered into clinical oncology trials.

in vitro

mk-4827displayed excellent parp 1 and 2 inhibition with ic50 of 3.8 and 2.1 nm, respectively. in a whole cell assay, mk-4827 inhibited parp activity with ec50 of 4 nm. mk-4827 also inhibited proliferation of cancer cells with mutant brca-1 and brca-2 with cc50 in the 10-100 nm range[1].

in vivo

in a variety of human tumor xenografts of differing p53 status,mk-4827 showed high potential to improve the efficacy of radiotherapy,such as calu-6 (p53 null), a549 (p53 wild-type [wt]) and h-460 (p53 wt) lung cancers and triple negative mda-mb-231 human breast carcinoma [3].

References

https://newdrugapprovals.org/2016/12/22/niraparib-mk-4827/
https://www.fda.gov/drugs/informationondrugs/approveddrugs/ucm548487.htm
https://www.drugbank.ca/drugs/DB11793
Sandhu, Shahneen K, et al. "The poly (ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA, mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial." Lancet Oncology14.9 (2013):882.
Jones, P, et al. "Niraparib: A Poly (ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination. " Journal of Medicinal Chemistry 58.8(2015):3302-14.

Niraparib Preparation Products And Raw materials

Raw materials

Preparation Products

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Niraparib Suppliers

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View Lastest Price from Niraparib manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.
Product
Niraparib 1038915-60-4
Price
US $0.00-0.00/g
Min. Order
10000g
Purity
99% HPLC
Supply Ability
1000kg
Release date
2024-09-11
ShenZhen H&D Pharmaceutical Technology Co., LTD
Product
Niraparib 1038915-60-4
Price
US $0.00-0.00/mg
Min. Order
10mg
Purity
0.98
Supply Ability
10g
Release date
2024-05-07
Nanjing Fred Technology Co., Ltd
Product
Niraparib 1038915-60-4
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%, Single impurity<0.1
Supply Ability
1 ton
Release date
2023-12-25

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