Saracatinib

Bezeichnung:Saracatinib

CAS-Nr379231-04-6

Englisch Name:Saracatinib

CBNumberCB61518531

SummenformelC27H32ClN5O5

Molgewicht542.03

MOL-Datei379231-04-6.mol

Saracatinib physikalisch-chemischer Eigenschaften

Schmelzpunkt	84-89°C
Siedepunkt	671.2±55.0 °C(Predicted)
Dichte	1.348
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (50 mg/ml) and ethanol (54 mg/mL with warming)
Aggregatzustand	solid
pka	7.55±0.10(Predicted)
Farbe	White
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Gefahreninformationscode (GHS)

Saracatinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC₅₀ = 2.7 and 30 nM, respectively). It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases. Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival. Through its effects on c-Src, it reduces osteoclast bone resorption. Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.
Chemische Eigenschaften
White Solid
Verwenden
An oral, selective dual inhibitor of Src and ABL kinase. It is a COVID19-related research product.
Definition
ChEBI: Saracatinib is a member of the class of quinazolines that is quinazoline substituted by (5-chloro-2H-1,3-benzodioxol-4-yl)amino, (oxan-4-yl)oxy and 2-(4-methylpiperazin-1-yl)ethoxy groups at positions 4, 5 and 7, respectively. It is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively). Saracatinib was originally developed by AstraZeneca for the treatment of cancer but in 2019 it was granted orphan drug designation by the US Food and Drug Administration for the treatment of idiopathic pulmonary fibrosis (IPF), a type of lung disease that results in scarring (fibrosis) of the lungs. It has a role as an antineoplastic agent, an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, a radiosensitizing agent, an autophagy inducer, an apoptosis inducer and an anticoronaviral agent. It is a member of quinazolines, a secondary amino compound, a N-methylpiperazine, an aromatic ether, a member of oxanes, a member of benzodioxoles, an organochlorine compound and a diether.
Lager
Store at -20°C
Einzelnachweise
Hennequin et al. (2006), N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor; J. Med. Chem., 49 6465 Green et al. (2009), Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530; Oncol., 3 248 de Wispelaere et al. (2013), The small molecules AZD0530 and Dasatinib inhibit dengue virus RNA replication via Fyn kinase; Virol., 87 7367 Shin et al. (2018), Saracatinib Inhibits Middle East Respiratory Syndrome-Coronavirus Replication In Vitro; Viruses, 10 283 Tang et al. (2020), Fyn kinase inhibition reduces protein aggregation, increases synapse density and improves memory in transgenic mice and traumatic Tauopathy; Acta Neuropathol. Commun., 8 96 Kaufman et al. (2015), Fyn inhibition rescues established memory and synapse loss in Alzheimer mice; Neurol., 77 953

Saracatinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

379231-04-6, Saracatinib Verwandte Suche:

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