Information TAS4464 TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. TAS4464 exhibits superior antitumor activity with prolonged target inhibition. Targets NAE (Cell-free assay) 0.955 nM In vitro TAS4464 selectively inhibits NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibits cullin neddylation and subsequently induces the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IkBa in human cancer cell lines. Cytotoxicity profiling reveals that TAS4464 is highly potent with widespread antiproliferative activity not only for cancer cell lines, but also patient-derived tumor cells. In vivo TAS4464 shows 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. Cell Research(from reference) Cell lines：PBMC, AML, DLBCL, SCLC cells. Patient-derived ovary and endometrial cells. Hepatocytes. Concentrations：1 nM, 10 nM, 100 nM, 1000 nM Incubation Time：24 h, 72 h, 6 days
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TAS4464
CAS number：1848959-10-3 molecular formula：C21H23FN6O6S
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| Chinese alias | - | ||
| English alias | 7H-Pyrrolo[2,3-d]pyrimidin-4-amine,7-[5-[(aminosulfonyl)amino]-5-deoxy-β-D-ribofuranosyl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]- | ||
| CAS number | 1848959-10-3 | molecular formula | C21H23FN6O6S |
| molecular weight | 506.51 g/mol | Exact mass | ≥98% |
| PSA | 196.000 Ų | logp | 0.200 |
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