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DD-03-171

Chemical Structure : DD-03-171

CAS No.: 2366132-45-6

DD-03-171

Catalog No.: PC-35884Not For Human Use, Lab Use Only.

DD-03-171 is a small molecule, CGI1746-based BTK degrader (PROTAC, biochemical IC50=5.1 nM) that efficiently degrade C481S-BTK, exhibits enhanced anti-proliferative effects on mantle cell lymphoma (MCL) cells in vitro by degrading BTK, IKFZ1 and IKFZ3.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DD-03-171 is a small molecule, CGI1746-based BTK degrader (PROTAC, biochemical IC50=5.1 nM) that efficiently degrade C481S-BTK, exhibits enhanced anti-proliferative effects on mantle cell lymphoma (MCL) cells in vitro by degrading BTK, IKFZ1 and IKFZ3; also displays efficacy against patient-derived xenografts in vivo.

Physicochemical Properties

M.Wt 991.163
Formula C55H62N10O8
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(tert-butyl)-N-(3-(6-((4-(4-(6-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamido)hexyl)piperazine-1-carbonyl)phenyl)amino)-4-methyl-5-oxo-4,5-dihydropyrazin-2-yl)-2-methylphenyl)benzamide

References

1. Dobrovolsky D, et al. Blood. 2018 Dec 13. pii: blood-2018-07-862953. doi: 10.1182/blood-2018-07-862953.

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