Chemical Properties | Back Directory | [Boiling point ]
738.0±60.0 °C(Predicted) | [density ]
1.347±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
10.70±0.40(Predicted) | [color ]
Light yellow to green yellow |
Hazard Information | Back Directory | [Uses]
Cemsidomide (CFT7455) is a ubiquitin ligase pathway Ikaros/Aiolos degrader with molecular glue activity[1]. Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells. | [in vivo]
In mouse xenograft tumor models, Cemsidomide demonstrates dose dependent efficacy from 3 μg/kg/day to 100 μg/kg/day. In several tumor xenografts tested daily dosing of Cemsidomide at dose of 30 μg/kg/day to 100 μg/kg/day led to durable tumor regression[1]. Cemsidomide (0.1 mg/kg/day; for 21 days) promotes tumor regression in the H929 tumor xenograft model (95% tumor growth inhibition by 7 days)[2]. | [IC 50]
Cereblon: 0.9 nM (Kd) | [References]
[1] David Proia, et al. Advantageous therapies for disorders mediated by ikaros or aiolos. WO2022032132A1. [2] James A. Henderson, et al. Abstract LB007: CFT7455: A novel, IKZF1/3 degrader that demonstrates potent tumor regression in IMiD-resistant multiple myeloma (MM) xenograft models. Cancer Res (2021) 81 (13_Supplement): LB007. |
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