MLN9708

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

MLN9708(1201902-80-8) is an orally bioavailable second generation proteasome inhibitor with potential antineoplastic activity. MLN9708(1201902-80-8) rapidly hydrolyzes to MLN2238, the biologically active form. It has a shorter proteasome dissociation half-life and improved pharmacokinetics, pharmacodynamics, and antitumor activity compared with bortezomib. It has a larger blood volume distribution at steady state, and analysis of 20S proteasome inhibition and markers of the unfolded protein response confirmed that MLN9708(1201902-80-8) has greater pharmacodynamic effects in tissues than bortezomib. MLN9708(1201902-80-8)showed activity in both solid tumor and hematologic preclinical xenograft models, and we found a correlation between greater pharmacodynamic responses and improved antitumor activity

参考文献

[1] http://www.cancer.gov/drugdictionary/?CdrID=635527

[2] http://ash.confex.com/ash/2010/webprogram/Paper31616.html