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High affinity PDEδ-KRAS interaction inhibitor (Kd = 41 nM); binds to PDEδ. Reduces proliferation and induces cell death of KRAS-dependent Panc-Tu-1 and Capan-1 pancreatic cancer cells. Attenuates tumor growth of Panc-Tu-1 xenografts in mice.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 713.14. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.4 mL||7.01 mL||14.02 mL|
|5 mM||0.28 mL||1.4 mL||2.8 mL|
|10 mM||0.14 mL||0.7 mL||1.4 mL|
|50 mM||0.03 mL||0.14 mL||0.28 mL|
References are publications that support the biological activity of the product.
Zimmermann et al (2013) Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature 497 638 PMID: 23698361
Zimmermann et al (2014) Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site. J.Med.Chem. 57 5435 PMID: 24884780
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Keywords: Deltarasin, Deltarasin supplier, high, affinity, PDEdelta, PDED, PDEδ, PDE6D, phosphodiesterases, KRAS, inhibitors, inhibits, Phosphodiesterases, Ras, GTPases, 5424, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
RAS Oncoproteins Scientific Review
Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.