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Niraparib

Niraparib Struktur
1038915-60-4
CAS-Nr.
1038915-60-4
Englisch Name:
Niraparib
Synonyma:
(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
Summenformel:
C19H20N4O
Molgewicht:
320.39
MOL-Datei:
1038915-60-4.mol

Niraparib Eigenschaften

Schmelzpunkt:
187-189°C
Siedepunkt:
463.6±45.0 °C(Predicted)
Dichte
1.34
storage temp. 
2-8°C(protect from light)
L?slichkeit
DMSO (Slightly), Methanol (Slightly)
pka
15.36±0.30(Predicted)
Aggregatzustand
Solid
Farbe
Pale Yellow to Light Yellow
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H332 Gesundheitssch?dlich bei Einatmen. Akute Toxizit?t inhalativ Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P261, P271, P304+P340, P312
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

Niraparib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

(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.

Verwenden

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

Pharmakologie

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.

Einzelnachweise

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

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

Downstream Produkte

Niraparib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 303)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
SyncoZymes (Shanghai) Co., Ltd., 		+86-021-68187180-811 +86-13681683526
 lchen@syncozymes.com China 188 58
Hebei Yanxi Chemical Co., Ltd. 		+8617531153977
 allison@yan-xi.com China 5857 58
Hebei Weibang Biotechnology Co., Ltd 		+8617732866630
 bess@weibangbio.com China 18148 58
HangZhou RunYan Pharma Technology Co.,LTD. 		+8618882027439
 sales2@runyanpharma.com China 302 58
Hangzhou ICH Biofarm Co., Ltd 		+86-0571-28186870; +undefined8613073685410
 sales@ichemie.com China 1010 58
Henan Fengda Chemical Co., Ltd 		+86-371-86557731 +86-13613820652
 info@fdachem.com China 20274 58
Capot Chemical Co.,Ltd. 		+86-（0）57185586718 +86-13336195806
 sales@capot.com China 29793 60
Beijing Cooperate Pharmaceutical Co.,Ltd 		010-60279497
sales01@cooperate-pharm.com CHINA 1803 55
Henan Tianfu Chemical Co.,Ltd. 		+86-0371-55170693 +86-19937530512
 info@tianfuchem.com China 21634 55
Hangzhou FandaChem Co.,Ltd. 		+8615858145714
 FandaChem@Gmail.com China 8779 55
  • 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
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