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DT204

Names

[ CAS No. ]:
428497-71-6

[ Name ]:
DT204

[Synonym ]:
(4-Bromo-2-{(Z)-[3-(4-chlorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}phenoxy)acetic acid
Acetic acid, 2-[4-bromo-2-[(Z)-[3-[(4-chlorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]-

Biological Activity

[Description]:

DT204 (DT-204) is a novel SCFSkp2 inhibitor that reduces Skp2 binding to Cullin-1 and Commd1, synergistically enhances BTZ-induced apoptosis; stablizes and increases p27 levels, does not increase the level of p53, demonstrates potential synergy with CI values of 0.7, 0.8 and 0.7 for RPMI8226, U266 and MM1.S respectively combined with 1 nM BTZ, co-treatment induces apoptosis in cells resistant to the proteasome inhibitors BTZ, carfilzomib or ixazomib; overcomes drug resistance and reduces the in vivo growth of myeloma tumors in murine models.

[References]

References 1. Malek E, et al. Leukemia. 2017 Mar;31(3):645-653. View Related Products by Target E3 Ubiquitin Ligase

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
647.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H13BrClNO5S

[ Molecular Weight ]:
482.732

[ Flash Point ]:
345.3±34.3 °C

[ Exact Mass ]:
480.938629

[ LogP ]:
5.13

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.719

Related Compounds