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Submit ReviewDeltarasin
Description: High affinity PDEδ-KRas interaction inhibitor; binds to PDEδ
Chemical Name: 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for Deltarasin
Deltarasin is a 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.
Compound Libraries for Deltarasin
Deltarasin is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Deltarasin
| M. Wt | 713.14 |
| Formula | C40H37N5O.3HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1440898-82-7 |
| PubChem ID | 91826089 |
| InChI Key | NCIOVAYUMQEQEU-VKZSUDIWSA-N |
| Smiles | C12=CC=CC=C1N=C(C4=CC=C(OC[C@H]([C@H]8CCNCC8)N5C(C7=CC=CC=C7)=NC6=C5C=CC=C6)C=C4)N2CC3=CC=CC=C3.Cl.Cl.Cl |
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.
Solubility Data for Deltarasin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 71.31 | 100 | |
| DMSO | 71.31 | 100 |
Preparing Stock Solutions for Deltarasin
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 |
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Product Datasheets for Deltarasin
References for Deltarasin
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
If you know of a relevant reference for Deltarasin, please let us know.
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Keywords: Deltarasin, Deltarasin supplier, high, affinity, PDEdelta, PDED, PDEδ, PDE6D, phosphodiesterases, KRAS, inhibitors, inhibits, Phosphodiesterases, Ras, GTPases, 5424, Tocris Bioscience
2 Citations for Deltarasin
Citations are publications that use Tocris products. Selected citations for Deltarasin include:
Rudolf A et al (2022) An In Vivo Inflammatory Loop Potentiates KRAS Blockade. Biomedicines 10 PMID: 35327394
Malcolm G et al (2022) RNA splicing is a key mediator of tumour cell plasticity and a therapeutic vulnerability in colorectal cancer. Nat Commun 13 2791 PMID: 35589755
Do you know of a great paper that uses Deltarasin from Tocris? Please let us know.
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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.
Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
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- Drivers of Metabolic Reprogramming
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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. 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
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.
Pathways for Deltarasin
Akt Signaling Pathway
The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.