1149705-71-4 Usage
Description
XL888 is a heat shock protein 90 (Hsp90) inhibitor, which plays a crucial role in maintaining the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis. As an ATP-competitive inhibitor of Hsp90, XL888 targets and degrades specific client proteins, leading to cell cycle arrest or apoptosis. It is orally bioavailable and has demonstrated efficacy in tumor regression in gastric carcinoma and melanoma xenografts in mice.
Uses
Used in Pharmaceutical Industry:
XL888 is used as an Hsp90 inhibitor for targeting and degrading specific client proteins, which results in cell cycle arrest or apoptosis. This action makes XL888 a potential therapeutic agent for cancer treatment, particularly in gastric carcinoma and melanoma.
Used in Cancer Research:
XL888 is used as a research tool for studying the role of Hsp90 in cancer cell proliferation, cell cycling, and apoptosis. Its ATP-competitive inhibition of Hsp90 allows researchers to investigate the underlying mechanisms of cancer development and progression, as well as the potential for targeted therapies.
Used in Drug Development:
XL888 is used as a lead compound in the development of novel Hsp90 inhibitors for cancer treatment. Its oral bioavailability and demonstrated efficacy in tumor regression make it a promising candidate for further optimization and development into more potent and selective Hsp90 inhibitors.
Used in Drug Delivery Systems:
XL888 can be used in the development of drug delivery systems to improve its pharmacokinetics, bioavailability, and therapeutic outcomes. By employing various organic and metallic nanoparticles as carriers, XL888's delivery can be enhanced, potentially leading to more effective cancer treatments.
Biological Activity
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1149705-71-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,4,9,7,0 and 5 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1149705-71:
(9*1)+(8*1)+(7*4)+(6*9)+(5*7)+(4*0)+(3*5)+(2*7)+(1*1)=164
164 % 10 = 4
So 1149705-71-4 is a valid CAS Registry Number.
