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BI-3663

Chemical Structure : BI-3663

CAS No.: 2341740-84-7

BI-3663 (BI3663;BI 3663)

Catalog No.: PC-36067Not For Human Use, Lab Use Only.

BI-3663 (BI 3663) is a cereblon-based degrader (PROTAC) of Focal adhesion tyrosine kinase (PTK2/FAK) with a median DC50 of 30 nM to >80% across a panel of eleven HCC cell lines.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BI-3663 (BI 3663) is a cereblon-based degrader (PROTAC) of Focal adhesion tyrosine kinase (PTK2/FAK) with a median DC50 of 30 nM to >80% across a panel of eleven HCC cell lines.
BI-3663 degraded PTK2 potently (DC50 = 27 nM) with a maximally obtainable degradation at the chosen experimental conditions of 95% (Dmax) in human lung adenocarcinoma cell line A549 after 16 hours treatment.
BI-3663 does not phenocopy the reported antiproliferative effects of PTK2 depletion in any of the cell lines tested.

Physicochemical Properties

M.Wt 917.84
Formula C44H42F3N7O12
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

N-(2-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3-oxopropoxy)ethoxy)ethoxy)ethyl)-3-methoxy-4-((4-((3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide

References

1. Popow J, et al. J Med Chem. 2019 Feb 9. doi: 10.1021/acs.jmedchem.8b01826.

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