Pevonedistat hydrochloride

Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC 50 of 4.7 nM In Vitro Pevonedistat (MLN4924) is a potent inhibitor of NAE (half-maximal inhibitory concentration (IC 50 =0.004 μM), and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC 50 =1.5, 8.2, 1.8 and >10 μM, respectively). Pevonedistat (MLN4924) treatment inhibits overall protein turnover in cultured HCT-116 cells. Treatment of HCT-116 cells with Pevonedistat (MLN4924) for 24 h results in a dose-dependent decrease of Ubc12-NEDD8 thioester and NEDD8-cullin conjugates, with an IC 50 In Vivo Pevonedistat (MLN492410, 30 or 60 mg/kg, s.c.) leads to a dose- and time-dependent increase in the steady state levels of NRF2 and CDT1 in HCT-116 tumour-bearing mice, and decreases NEDD8-cullin levels in normal mouse tissue as illustrated in mouse bone marrow cells. Pevonedistat (MLN4924) administered on a BID schedule at 30 and 60 mg/kg inhibits tumour growth with T/C values of 0.36 and 0.15, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 4.7 nM (NAE)

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