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KTX207

Chemical Structure : KTX207

CAS No.: 3075021-91-6

KTX207 (KTX-207)

Catalog No.: PC-24472Not For Human Use, Lab Use Only.

KTX207 is a potent, selective BI 1015550-based PDE4 PROTAC degrader, degrades PDE4D and PDE4B shortforms in A549 cells with IC50 of 10 pM and 400 pM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KTX207 is a potent, selective BI 1015550-based PDE4 PROTAC degrader, degrades PDE4D and PDE4B shortforms in A549 cells with IC50 of 10 pM and 400 pM, respectively.
KTX207 is highly selective for PDE4 shortforms over longforms.
KTX207 degrades PDE4D shortform with high selectivity at sub-nanomolar concentration via the ubiquitin-proteasomal system
KTX207 is more effective at increasing cAMP levels than conventional inhibitor BI 1015550.
KTX207 can suppress cancer cell growth in 2D and 3D cultures of A549 cells.

Physicochemical Properties

M.Wt 882.14
Formula C47H63N9O6S
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
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Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(5-(1-(9-((2-(1-((S)-4-((1-(hydroxymethyl)cyclobutyl)amino)-5-oxido-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperidin-4-yl)pyrimidin-5-yl)oxy)nonyl)piperidin-4-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

References

1. Sin YY. Et al. FEBS J. 2024 Dec 13. doi: 10.1111/febs.17359.

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