tas4464-hydrochloride

Description: TAS4464 (hydrochloride) is a novel, highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM, showing superior antitumor activity with prolonged target inhibition. TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 showed prolonged target inhibition in human tumor xenograft mouse models; weekly or twice a week TAS4464 administration led to prominent antitumor activity in multiple human tumor xenograft mouse models including both hematologic and solid tumors without marked weight loss. It is a promising agent for the treatment of a variety of tumors including both hematologic and solid tumors.

References: TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, suppresses neddylation and shows antitumor activity in diverse cancer models. Mol Cancer Ther. 2019 May 15.

Related CAS#: 1848959-11-4 (HCl); 1848959-10-3 (free base)