KX2-391

Bezeichnung:KX2-391

CAS-Nr897016-82-9

Englisch Name:KX2-391

CBNumberCB02561484

SummenformelC26H29N3O3

Molgewicht431.53

MOL-Datei897016-82-9.mol

KX2-391 physikalisch-chemischer Eigenschaften

Siedepunkt	680.9±55.0 °C(Predicted)
Dichte	1.169
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; ≥121 mg/mL in DMSO; ≥2.44 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	Powder
pka	14.73±0.46(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

KX2-391 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
A synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase inhibitor with an IC50 of average 72 nM.
Verwenden
KX2-391 is a Src Inhibitor with efficacy against certain hepatic and leukemia cell lines.
Biologische Aktivität
kx2-391 is a highly selective inhibitor of src kinase with ic50 value of 20nm [1].kx2-391 is a non-atp competitive inhibitor of src. it is the first inhibitor that targets src kinase within the substrate binding site. kx2-391 inhibits src catalyzed trans-phosphorylation of fak, shc, paxillin as well as src kinase autophosphorylation. kx2-391 has no effects on pdgfr, egfr, jak1, jak2 and lck demonstrating it as a selective inhibitor. it is also found to be an inhibitor of tubulin polymerization through binding to the unique confirmation on heterodimeric tubulin. in cellular assays, kx2-391 shows growth inhibition in nih3t3/c-src527f cells and syf/c-src527f cells with gi50 values of 23nm and 39nm, respectively [1, 2].since src acts as a regulator in cell proliferation survival, motility and invasiveness, kx2-391 is potent against a variety of solid tumors and many leukemia tumors. it is shown to inhibit primary tumor growth and to suppress metastasis [2].
target
Src (HuH7)
Einzelnachweise
[1] fallah-tafti a, foroumadi a, tiwari r, et al. thiazolyl n-benzyl-substituted acetamide derivatives: synthesis, src kinase inhibitory and anticancer activities. european journal of medicinal chemistry, 2011, 46(10): 4853-4858.
[2] naing a, cohen r, dy g k, et al. a phase i trial of kx2-391, a novel non-atp competitive substrate-pocket-directed src inhibitor, in patients with advanced malignancies. investigational new drugs, 2013, 31(4): 967-973.

KX2-391 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

897016-82-9, KX2-391 Verwandte Suche:

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