CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism [1].
In Vivo, CMLD010509 (0.7 mg/kg, i.p., twice a week) markedly reduces the tumor burden in MMIS xenograft SCID mouse model[1].
In Vitro, CMLD010509 exerts potent inhibitory activity against most multiple myeloma (MM) cell lines with IC50 values less than 10 nM[1]. CMLD010509 (100 nM, 2 h) disrupts the oncogenic translation program in NCI-H929 cells[1]. CMLD010509 (0-1000 nM, 3-24 h) strongly induces an apoptotic response in NCl-H929 and MM1S cells, as measured by caspase-3 and caspase-7 activation[1].
References:
[1]. Manier S, et al. Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Sci Transl Med. 2017 May 10;9(389). pii: eaal2668.
In Vivo, CMLD010509 (0.7 mg/kg, i.p., twice a week) markedly reduces the tumor burden in MMIS xenograft SCID mouse model[1].
In Vitro, CMLD010509 exerts potent inhibitory activity against most multiple myeloma (MM) cell lines with IC50 values less than 10 nM[1]. CMLD010509 (100 nM, 2 h) disrupts the oncogenic translation program in NCI-H929 cells[1]. CMLD010509 (0-1000 nM, 3-24 h) strongly induces an apoptotic response in NCl-H929 and MM1S cells, as measured by caspase-3 and caspase-7 activation[1].
References:
[1]. Manier S, et al. Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Sci Transl Med. 2017 May 10;9(389). pii: eaal2668.