Niraparib
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- 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;Niraparib;EOS-60867;Niraparib base;MK4827 (Niraparib);Niraparib USP/EP/BP;MK 4827;MK-4827;MK4827
- CBNumber:
- CB82514860
- Summenformel:
- C19H20N4O
- Molgewicht:
- 320.39
- MOL-Datei:
- 1038915-60-4.mol
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Niraparib Eigenschaften
- Schmelzpunkt:
- 187-189°C
- Siedepunkt:
- 463.6±45.0 °C(Predicted)
- Dichte
- 1.34
- storage temp.
- 2-8°C(protect from light)
- Löslichkeit
- DMSO (Slightly), Methanol (Slightly)
- pka
- 15.36±0.30(Predicted)
- Aggregatzustand
- Solid
- Farbe
- Pale Yellow to Light Yellow
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitsschädlich bei Verschlucken. |
Akute Toxizität oral |
Kategorie 4 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/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 pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
| H332 |
Gesundheitsschädlich bei Einatmen. |
Akute Toxizität inhalativ |
Kategorie 4 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P261, P271, P304+P340, P312 |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizität (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
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| 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 Möglichkeit entfernen. Weiter spülen. |
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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
Downstream Produkte
Niraparib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 283)Lieferanten
- 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%
- 1038915-60-4
- Anti-cancer&immunity
- API
