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Deltasonamide 1 TFA

Names

[ CAS No. ]:
2235358-73-1

[ Name ]:
Deltasonamide 1 TFA

Biological Activity

[Description]:

Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

[Target]

KD: 203 pM (PDE6δ-KRas)[1]


[In Vitro]

Deltasonamide 1 可以抑制 PDE6δ-KRas,KD 为 203 pM[1]。 Deltasonamide 1 通过多达 7 个氢键与 PDE6δ 结合,产生皮摩尔亲和力[1]。 Deltasonamide 1 强烈减少增殖[1]。 Cell Proliferation Assay[1] Cell Line: RTCA of hPDAC cell lines Concentration: 0.375, 0.75, 1.5, 3, 6, 12 μM Incubation Time: 60 h Result: Inhibited proliferation of human pancreatic cancer cell lines.

[References]

[1]. Pablo Martín-Gago, et al. A PDE6δ-KRas Inhibitor Chemotype With Up to Seven H-Bonds and Picomolar Affinity That Prevents Efficient Inhibitor Release by Arl2. Angew Chem Int Ed Engl. 2017 Feb 20;56(9):2423-2428.  

Chemical & Physical Properties

[ Molecular Formula ]:
C32H40ClF3N6O6S2

[ Molecular Weight ]:
761.27


Related Compounds