Supplier Related Products Identification Questions And Answer Chemical Properties Hazard Information
WebSite >  CAS DataBase List  > 1038915-60-4

1038915-60-4

Supplier Related Products Identification Questions And Answer Chemical Properties Hazard Information

Product Image

Identification

Name
Niraparib
CAS
1038915-60-4
Synonyms
Niraparib
EOS-60867
MK4827 (Niraparib)
Niraparib (MK-4827)
2-[4-(3S)piperidin-3-ylphenyl]-2H-indazol-7-carboxamide
2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-
2-[4-((3S)-3-Piperidinyl)phenyl]-2H-indazole-7-carboxamide
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide
MK-4827,(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrocholoride
Molecular Formula
C19H20N4O
MDL Number
MFCD17779309
Molecular Weight
320.388
MOL File
1038915-60-4.mol

Questions And Answer

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

Chemical Properties

Boiling point 
463.6±45.0 °C(Predicted)
density 
1.34
storage temp. 
Keep in dark place,Sealed in dry,2-8°C
pka
15.36±0.30(Predicted)

Hazard Information

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.
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.
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.
SupplierMore