SGX-523

Bezeichnung:SGX-523

CAS-Nr1022150-57-7

Englisch Name:SGX-523

CBNumberCB42501000

SummenformelC18H13N7S

Molgewicht359.41

MOL-Datei1022150-57-7.mol

SGX-523 physikalisch-chemischer Eigenschaften

Dichte	1.485
storage temp.	Store at -20°C
Löslichkeit	≥17.95 mg/mL in DMSO
pka	3.94±0.10(Predicted)
Aggregatzustand	solid

SGX-523 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
SGX523 is a novel, ATP-competitive kinase inhibitor.
Definition
ChEBI: A member of the class of triazolopyridazines that is 6-(1-methylpyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazine-3-thiol in which the thiol hydrogen is replaced by a quinolin-6-yl group.
Biologische Aktivität
sgx-523 is a novel, potent, atp-competitive, and highly-selective hepatocyte growth factor receptor (met) inhibitor with ic50 value of 4 nm [1].sgx523 inhibits met autophosphorylation in gastric cancer cell line gtl16 and human lung carcinoma cell line a549, with ic50 of 40 nm and 12 nm, respectively [1]. additionally, tumor regression was observed in gastic cancer cell line gtl16 and human gbm cell line u87mg derived mouse xenograft models that are treated with sgx-523 by oral gavage [1].sgx523 has been shown to inhibit the phosphorylateion of mek, mapk, akt in brain cancer cell lines including u87, u373, daoy, as well as glioma stem cells 1228. the inhibition of mek in brain cancer cells and stem cells led to cell proliferation, g1/s cell cycle progression, cell migration, and cell invasion [2].
Lager
Store at +4°C
Einzelnachweise
[1] buchanan sg1, hendle j, lee ps, smith cr, bounaud py, jessen ka, tang cm, huser nh, felce jd, froning kj, peterman mc, aubol be, gessert sf,sauder jm, schwinn kd, russell m, rooney ia, adams j, leon bc, do th, blaney jm, sprengeler pa, thompson da, smyth l, pelletier la, atwell s, holme k,wasserman sr, emtage s, burley sk, reich sh. sgx523 is an exquisitely selective, atp-competitive inhibitor of the met receptor tyrosine kinase with antitumor activity in vivo. mol cancer ther. 2009 dec;8(12):3181-90.
[2] guessous f1, zhang y, dipierro c, marcinkiewicz l, sarkaria j, schiff d, buchanan s, abounader r.an orally bioavailable c-met kinase inhibitor potently inhibits brain tumor malignancy and growth. anticancer agents med chem. 2010 jan;10(1):28-35.

SGX-523 Upstream-Materialien And Downstream Produkte

SGX-523 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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