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Nirogacestat

Nirogacestat Struktur
1290543-63-3
CAS-Nr.
1290543-63-3
Englisch Name:
Nirogacestat
Synonyma:
Nirogacestat;CS-2699;PF-3084014;PF-03084014 (PF-3084014);Nirogacestat (PF-03084014;PF-03084014 (Nirogacestat);Nirogacestat, 10 mM in DMSO;PF03084014;PF 03084014;PF-03084014;Nirogacestat(PF-03084014,PF-3084014);Nirogacestat,γ-secretase,Gamma secretase,cancer,inhibit,PF 3084014,gastrointestinal,toxicity,Inhibitor,Notch,PF3084014,Apoptosis
CBNumber:
CB42628246
Summenformel:
C27H41F2N5O
Molgewicht:
489.64
MOL-Datei:
1290543-63-3.mol

Nirogacestat Eigenschaften

Siedepunkt:
651.3±55.0 °C(Predicted)
Dichte
1.16±0.1 g/cm3(Predicted)
storage temp. 
room temp
L?slichkeit
Water:1.0(Max Conc. mg/mL);2.04(Max Conc. mM)
Aggregatzustand
powder
pka
13.27±0.70(Predicted)
Farbe
white to beige
Wasserl?slichkeit
H2O: 1mg/mL, clear
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
HS Code  29332900
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
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
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
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.
P337+P313 Bei anhaltender Augenreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.

Nirogacestat Chemische Eigenschaften,Einsatz,Produktion Methoden

Biochem/physiol Actions

PF-03084014 inhibits the Notch signalling pathway. It contributes totumor suppression in breast, pancreatic carcinoma, hepatocellular carcinoma and progressive desmoid tumors. PF-03084014 in combination with dexamethasone elicits antileukemic effects in T-cell acute lymphoblastic leukemias (T-ALL).

Enzyminhibitor

This novelγ-secretase inhibitor (FW = 489.66 g/mol; CAS 1290543-63-3; soluble in DMSO), also code-named HY-15185 and systematically named [(S)-2-((S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2- methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide], inhibitsγ-secretase reversibly, noncompetitively, and selectively, thereby reducing amyloid-b (Ab) production, with an in vitro IC50 of 1.2 nM in a whole-cell assay and 6.2 nM in cell-free assay. PF-03084014 inhibits Notch-related T- and B-cell maturation in an in vitro thymocyte assay with an EC50 of 2.1 μM. PF-3084014 had an IC50 on B- and T-cell reductions of 1.3 to 3 μM with a mean EC50 of 2.1 μM. This represents >300-fold separation from the broken-cell Aβ IC50 and >1500x separation from the whole-cell IC50. A single acute dose showed dose-dependent reduction in brain, cerebrospinal fluid (CSF), and plasma Ab . When dosed with PF- 3084014 for 5 days using an osmotic minipump (0.03 to 3 mg/kg/day), Guinea pigs exhibited dose-dependent Ab reduction in brain, CSF, and plasma. While otherγ-secretase inhibitors show high potency at elevating Ab in the conditioned media of whole cells and the plasma of multiple animal models and humans, such potentiation is not observed with PF- 3084014. By evoking antitumor and antimetastatic properties via pleiotropic mechanisms, experiments with PF-03084014 offer hope that Notch pathway downstream genes may be used to predict the antitumor activity of PF-03084014 in breast cancer patients.

Nirogacestat Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Nirogacestat Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 110)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 33024 60
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19552 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49732 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58
Nantong HI-FUTURE Biology Co., Ltd.
+undefined18051384581
sales@chemhifuture.com China 3135 58
TargetMol Chemicals Inc.

support@targetmol.com United States 38669 58
Chemtour Biotech Co., Ltd
+8617327281506
market@chemtour.com China 1521 58
Wuhan Topule Biopharmaceutical Co., Ltd
+8618327326525
masar@topule.com China 8467 58
Shanghai Acmec Biochemical Technology Co., Ltd.
+86-18621343501; +undefined18621343501
product@acmec-e.com China 33338 58

  • (S)-2-((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide Molecular Weight: 489.64
  • PF-03084014 (PF-3084014)
  • PF-3084014
  • (2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-N-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide
  • PF03084014;PF 03084014;PF-03084014
  • CS-2699
  • PF-03084014 (Nirogacestat)
  • Nirogacestat(PF-03084014,PF-3084014)
  • Pentanamide, 2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-N-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1H-imidazol-4-yl]-, (2S)-
  • Nirogacestat (PF-03084014
  • Nirogacestat
  • Nirogacestat,γ-secretase,Gamma secretase,cancer,inhibit,PF 3084014,gastrointestinal,toxicity,Inhibitor,Notch,PF3084014,Apoptosis
  • Nirogacestat, 10 mM in DMSO
  • 1290543-63-3
  • api
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