Deltarasin

Pricing Availability   Qty
Cat.No. 5424 - Deltarasin | C40H37N5O.3HCl | CAS No. 1440898-82-7
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

Deltarasin is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 71.31 100
DMSO 71.31 100

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 solvent 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References

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.

Keywords: Deltarasin, Deltarasin supplier, high, affinity, PDEdelta, PDED, PDEδ, PDE6D, phosphodiesterases, KRAS, inhibitors, inhibits, Phosphodiesterases, Ras, 5424, Tocris Bioscience

Citations for Deltarasin

Citations are publications that use Tocris products.

Currently there are no citations for Deltarasin. Do you know of a great paper that uses Deltarasin from Tocris? Please let us know.

Reviews for Deltarasin

There are currently no reviews for this product. Be the first to review Deltarasin and earn rewards!

Have you used Deltarasin?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
RAS Oncoproteins

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

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

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.