产品描述

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.

靶点活性

20S proteasome β5    20S proteasome β1    20S proteasome β2

体外活性

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].

体内活性

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].

别名

化合物Ixazomib citrate , MLN9708 , 枸橼酸艾沙佐米

纯度

98%

分子量

517.12

分子式

C20H23BCl2N2O9

CAS No.

1239908-20-3

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 100 mg/mL (193.38 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Note

For research use only.