mln9708

MLN9708 (Ixazomib Citrate) 抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点 (Ki50=0.93 nM, IC50=3.4 nM )。 MLN9708 的生物活性形式是水溶液或血浆中的 MLN2238。

VPC-16606 is a potent and selective inhibitor of ERα-dependent cell growth and gene expression. VPC-16606 prevents the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner.

Ixazomib citrate (MLN9708) 是 Ixazomib 的前药，是20S 蛋白酶体胰凝乳蛋白酶样蛋白水解β5位点的可逆抑制剂，IC50为3.4 nM 和Ki 为0.93 nM。

Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrolyzing to pharmacologically active MLN2238 (ixazomib), is a next-generation proteasome inhibitor with demonstrated preclinical and clinical antimyeloma activity. MLN9708, compared with bortezomib, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinical studies.