Ixazomib citrate 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 is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (IC50 of 3.4 nM ) with potential antineoplastic activity.

Treatment of MM cells with MLN2238 predominantly inhibits chymotrypsin-like activity of the proteasome and induces accumulation of ubiquitinated proteins. MLN2238 inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies without affecting the viability of normal cells[1].

In animal tumor model studies, MLN2238 is well tolerated and inhibits tumor growth with significantly reduced tumor recurrence. A head-to-head analysis of MLN2238 versus bortezomib showed a significantly longer survival time in mice treated with MLN2238 than mice receiving bortezomib[1].

1239908-20-3

C20H23BCl2N2O9

517.12

MLN9708;枸橼酸艾沙佐米

DMSO:100 mg/mL (193.38 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years