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Deltarasin

Chemical Structure : Deltarasin

CAS No.: 1440898-61-2

Deltarasin

Catalog No.: PC-22366Not For Human Use, Lab Use Only.

Deltarasin is potent, specfic inhibitor of KRAS-PDEδ (PDE6D) interaction, bind to the prenyl-binding pocket of PDEδ with KD of 38 nM, inhibits oncogenic RAS signalling.

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

Biological Activity

Deltarasin is potent, specfic inhibitor of KRAS-PDEδ (PDE6D) interaction, bind to the prenyl-binding pocket of PDEδ with KD of 38 nM, inhibits oncogenic RAS signalling.
Deltarasin interferes with the binding of KRAS to PDEδ in cells and resulting delocalization of KRAS.
Deltarasin potently suppresses proliferation and MAPK-signalling in oncogenic KRAS-dependent PDAC cells.
Deltarasin (10 mg/kg QD, 15 mg/ kg QD and 10 mg/kg BID) impairs dose-dependent in vivo growth of xenografted pancreatic carcinoma in nude mice.

Physicochemical Properties

M.Wt 603.77
Formula C40H37N5O
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

(S)-1-Benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole

References

1. Leung ELH, et al. Cell Death Dis. 2018 Feb 13;9(2):216.

2. Agalioti T, et al. Nat Commun. 2017 May 16;8:15205.

3. Papke B, et al. Nat Commun. 2016 Apr 20;7:11360.

4. Zimmermann G, et al. Nature. 2013 May 30;497(7451):638-42.

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