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Niraparib

Niraparib Structure
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
Molecular Weight:
320.39
MOL File:
1038915-60-4.mol
MSDS File:
SDS
Modify Date:
2024/5/7 20:25:49
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Niraparib Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H332-H335
Precautionary statements  P261-P280-P305+P351+P338

Niraparib Chemical Properties,Uses,Production

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.

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.

Niraparib Preparation Products And Raw materials

Raw materials

MK-4827 (R-enantioMer) methyl 2-(4-(1-(tert-butoxycarbonyl)piperidin-3-yl)phenyl)-2H-indazole-7-carboxylate Niraparib intermediate 1 methyl 2-{4-[(3S)-1-(tert-butoxycarbonyl)piperidin-3-yl]-phenyl}-2H-indazole-7-carboxylate 2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrochloride
MK-4827 (tosylate) Methyl 3-formyl-2-nitrobenzoate
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Preparation Products

Niraparib Suppliers

Global( 288)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Jigs Chemical ltd +919099003427 Gujarat, India 239 58 Inquiry
Bulat Pharmaceutical Pvt Ltd +91-8448085659 +91-8448085660 Haryana, India 123 58 Inquiry
AKASH PHARMA EXPORTS +91-9388123451 +91-9846039283 Kerela, India 470 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
SyncoZymes (Shanghai) Co., Ltd., +86-021-68187180-811 +86-13681683526 China 188 58 Inquiry
Hebei Yanxi Chemical Co., Ltd. +86-17531190177; +8617531190177 China 6011 58 Inquiry
Hangzhou ICH Biofarm Co., Ltd +86-0571-28186870; +undefined8613073685410 China 985 58 Inquiry
Supplier Advantage
Jigs Chemical ltd 58
Bulat Pharmaceutical Pvt Ltd 58
AKASH PHARMA EXPORTS 58
CLEARSYNTH LABS LTD. 58
A.J Chemicals 58
Pharmaffiliates Analytics and Synthetics P. Ltd 58
SynZeal Research Pvt Ltd 58
SyncoZymes (Shanghai) Co., Ltd., 58
Hebei Yanxi Chemical Co., Ltd. 58
Hangzhou ICH Biofarm Co., Ltd 58

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MK-4827,(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide Niraparib 2-[4-((3S)-3-Piperidinyl)phenyl]-2H-indazole-7-carboxamide MK4827 (Niraparib) 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]- (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrocholoride 2-[4-(3S)piperidin-3-ylphenyl]-2H-indazol-7-carboxamide 2-[4-[(3s)-piperidin-3-yl]phenyl]indazole-7-carboxamide CS-2299 MK 4827;MK-4827;MK4827 Niraparib(MK4827) free base EOS-60867 Niraparib base Niraparib USP/EP/BP Best Price API 99% CAS?1038915-60-4?Niraparib Powder Niraparib D4Q: What is Niraparib D4 Q: What is the CAS Number of Niraparib D4 (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide Niraparib (MK-4827) MK-4827 98.00% iraparib 1038915-60-4 Anti-cancer&immunity API