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BGB-16673

Chemical Structure : BGB-16673

CAS No.: 2736508-94-2

BGB-16673 (BGB16673)

Catalog No.: PC-21567Not For Human Use, Lab Use Only.

BGB-16673 is an orally available heterobifunctional BTK PROTAC degrader that binds to BTK and E3 ligase, degrades wildtype BTK and multiple mutant forms via ubiquitination.

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Purity & Documentation Purity: 99.7% (HPLC) Select Batch:

Biological Activity

BGB-16673 is an orally available heterobifunctional BTK PROTAC degrader that binds to BTK and E3 ligase, degrades wildtype BTK and multiple mutant forms via ubiquitination.
BGB-16673 exhibits high potency on clinically relevant BTK mutants resistant to covalent and non-covalent BTK inhibitors in cancer cells in vitro.
BGB-16673 drives complete tumor regression of lymphoma xenograft models expressing wildtype or BTK mutations resistant to covalent and non-covalent inhibitors.
BGB-16673 presents longer duration of response than BTK inhibitors in BTK wildtype and C481S mutant-expressing lymphoma xenograft models.

Physicochemical Properties

M.Wt 850.04
Formula C48H55N11O4
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

3-(tert-butyl)-N-((1R)-1-(4-(6-(6-(4-((1-(4-(2,6-dioxopiperidin-3-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)pyridin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-methylphenyl)ethyl)-1,2,4-oxadiazole-5-carboxamide

References

1. John F. Seymour, et al. Blood (2023) 142 (Supplement 1): 4401.

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