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Deltaflexin3

Chemical Structure : Deltaflexin3

CAS No.: 2767277-64-3

Deltaflexin3 (Deltaflexin 3)

Catalog No.: PC-22365Not For Human Use, Lab Use Only.

Deltaflexin3 is a highly potent, selective and highly soluble inhibitor of the trafficking chaperone PDE6D (PDEδ) with KD value of 6 nM, inhibits PDE6D/K-Ras binding and KRAS mutant cancer cell growth.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Deltaflexin3 is a highly potent, selective and highly soluble inhibitor of the trafficking chaperone PDE6D (PDEδ) with KD value of 6 nM, inhibits PDE6D/K-Ras binding and KRAS mutant cancer cell growth.
Deltaflexin3 displays good selectivity for PDE6D-dependent and KRAS mutant with EC50 of 6 uM for MIA PaCa-2 (KRAS-G12C mutant) cells, as compared to HRAS mutant cancer cell lines.
Deltaflexin3 with the approved drug Sildenafil synergistically inhibit intracellular binding of K-Ras to PDE6D, more potently inhibits Ras signaling and microtumor growth.

Physicochemical Properties

M.Wt 457.59
Formula C25H36FN5O2
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-(7-(ethyl((2-(methylamino)pyrimidin-4-yl)methyl)amino)-7-oxoheptyl)-4-fluoro-N-isopropylbenzamide

References

1. Pelin Kaya, et al. J Med Chem. 2024 May 17. doi: 10.1021/acs.jmedchem.3c02129.

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