AMG 925 Struktur

AMG 925

Bezeichnung:AMG 925

CAS-Nr1401033-86-0

Englisch Name:AMG 925

CBNumberCB32685918

SummenformelC26H29N7O2

Molgewicht471.55

MOL-Datei1401033-86-0.mol

AMG 925 physikalisch-chemischer Eigenschaften

Siedepunkt	712.3±70.0 °C(Predicted)
Dichte	1.48±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in DMSO; insoluble in H2O; insoluble in EtOH
Aggregatzustand	solid
pka	13.41±0.10(Predicted)
Farbe	Light yellow to yellow

AMG 925 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4; IC₅₀s = 1 and 3 nM, respectively). It is selective for FLT3 and Cdk4 over Cdk1 (IC₅₀ = 2.22 μM). AMG 925 also binds to FLT3^ITD, FLT3^D835Y, FLT3^D835H, FLT3^K663Q, and FLT3^N841I (K_ds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC₅₀s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.
Verwenden
AMG 925 is a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3.
Definition
ChEBI: AMG-925 is an organic heterotricyclic compound that is 9H-pyrido[4',3':4,5]pyrrolo[2,3-d]pyrimidine which is substituted by a [6-(hydroxyacetyl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-yl]nitrilo group at position 2 and by a trans-4-methylcyclohexyl group at position 9. It is a FLT3 and CDK4 dual kinase inhibitor that has antineoplastic activity. Currently under clinical investigation in patients with relapsed or refractory acute myeloid leukemia (AML). It has a role as an antineoplastic agent, an apoptosis inducer, an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a secondary amino compound, a tertiary amino compound, a naphthyridine derivative, a primary alpha-hydroxy ketone and an organic heterotricyclic compound.
target
FLT3
Einzelnachweise
[1] keegan k, li c, li z, ma j, ragains m, coberly s, hollenback d, eksterowicz j, liang l, weidner m, huard j, wang x, alba g, orf j, lo mc, zhao s, ngo r, chen a, liu l, carlson t, quéva c, mcgee lr, medina j, kamb a, wickramasinghe d, dai k. preclinical evaluation of amg 925, a flt3/cdk4 dual kinase inhibitor for treating acute myeloid leukemia. mol cancer ther. 2014 apr;13(4):880-9.

AMG 925 Upstream-Materialien And Downstream Produkte

AMG 925 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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