XL888

Bezeichnung:XL888

CAS-Nr1149705-71-4

Englisch Name:XL888

CBNumberCB42570387

SummenformelC29H37N5O3

Molgewicht503.64

MOL-Datei1149705-71-4.mol

XL888 physikalisch-chemischer Eigenschaften

Siedepunkt	695.1±55.0 °C(Predicted)
Dichte	1.27±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; insoluble in EtOH; ≥18.2 mg/mL in DMSO
Aggregatzustand	solid
pka	14.33±0.20(Predicted)
Farbe	Off-white to light yellow

Gefahreninformationscode (GHS)

XL888 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
XL888, is a heat shock protein 90 (Hsp90) inhibitor. HSP90, is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis.1 XL888 is an ATP-competitive inhibitor of Hsp90.2 Through this action, specific client proteins are degraded, resulting in cell cycle arrest or apoptosis.3,4,5 XL888 is orally bioavailable and shows efficacy in tumor regression in gastric carcinoma and melanoma xenografts in mice
Biologische Aktivität
xl-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (hsp90) that selectively inhibits hsp90α and hsp90β with values of 50% inhibition concentration ic50 of 22 nm and 44 nm respectively. it also exerts considerably weaker inhibition against a range of other diverse kinases with ic50 more than 3600 nm for all. x-ray crystallographic analysis reveals that the xl-888 binds to hsp90 through the formation of h-bonding between the n-(r)-sec-butylanthranilamide moiety of xl-888 and asp93 of hsp90. in recent studies, xl-888 has exhibits strong anti-proliferative activities in a panel of tumor cells with values of ic50 ranging from 0.1 nm to 45.5 nm.paraiso kh, haarberg he, wood e, rebecca vw, chen ya, xiang y, ribas a, lo rs, weber js, sondak vk, john jk, sarnaik aa, koomen jm, smalley ks. the hsp90 inhibitor xl888 overcomes braf inhibitor resistance mediated through diverse mechanisms. clin cancer res. 2012; 18(9):2502-2514bussenius j, blazey cm, aay n, anand nk, arcalas a, baik t, bowles oj, buhr ca, costanzo s, curtis jk, defina sc, dubenko l, heuer ts, huang p, jaeger c, joshi a, kennedy ar, kim ai, lara k, lee j, li j, lougheed jc, ma s, malek s, manalo jc, martini jf, mcgrath g, nicoll m, nuss jm, pack m, peto cj, tsang th, wang l, womble sw, yakes m, zhang w, rice kd. discovery of xl888: a novel tropane-derived small molecule inhibitor of hsp90. bioorg med chem lett. 2012; 22(17): 5396-5404.
target
Hsp90

XL888 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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