AZD-4547

Bezeichnung:AZD-4547

CAS-Nr1035270-39-3

Englisch Name:AZD-4547

CBNumberCB92546547

SummenformelC26H33N5O3

Molgewicht463.57

MOL-Datei1035270-39-3.mol

AZD-4547 physikalisch-chemischer Eigenschaften

Schmelzpunkt	168-170°C
Siedepunkt	621.7±55.0 °C(Predicted)
Dichte	1.189
storage temp.	Refrigerator
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
pka	13.66±0.10(Predicted)
Aggregatzustand	Solid
Farbe	Pale Yellow to Light Beige

Gefahreninformationscode (GHS)

AZD-4547 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
AZD 4547 is a selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinase with IC₅₀ values of 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively. It displays weaker activity against FGFR4 (IC₅₀ = 165 nM), VEGFR2 (IC₅₀ = 24 nM), and a panel of other tyrosine and serine/theronine kinases such as insulin-like growth factor 1 receptor (IC₅₀ = 581 nM), cyclin-dependent kinase 2 (IC₅₀ = >10 μM), and p38 (IC₅₀ = >100 μM). AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC₅₀s = 18-281 nM). In an FGFR-driven human tumor xenograft mouse model, oral administration of AZD 4547 at concentrations up to 12.5 mg/kg/day resulted in potent dose-dependent antitumor activity.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
AZD4547 is a bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinases. AZD4547 is particularly effective in inhibiting FGFR1, 2, and 3 tyrosine k inases and is under clinical investigation for the treatment of FGFR-dependent tumors.
Definition
ChEBI: AZD4547 is a member of the class of benzamides that is a carboxamide resulting from the formal condensation of the carboxy group of 4-(cis-3,5-dimethylpiperazin-1-yl)benzoic acid with the amino substituent of 5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-amine. It is an inhibitor of the fibroblast growth factor receptor (FGFR). It has a role as a fibroblast growth factor receptor antagonist. It is a member of pyrazoles, a N-arylpiperazine and a member of benzamides.
target
FGFR1
Lager
Store at -20°C

AZD-4547 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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