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Deltarasin

Catalog No. T6462   CAS 1440898-61-2

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

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Deltarasin Chemical Structure
Deltarasin, CAS 1440898-61-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
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1 mL * 10 mM (in DMSO) In stock $ 163.00
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Purity: 99.06%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Targets&IC50 PDEδ:38 nM(Kd)
In vitro In liver cells, Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by Deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS. [1]
In vivo Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumor cell xenografts [1]. The finding may inspire novel drug discovery efforts aimed at the development of drugs targeting oncogenic RAS.
Kinase Assay Kd?values are measured by fluorescence polarization measurements. For direct titrations, increasing amounts of PDEδ are added to a solution containing 50-100?nM labelled small molecule in 200?μL PBS buffer. For displacement titrations, increasing amounts of the small molecules in DMSO are directly added to fluorescein-labelled atorvastatin (24?nM) and His6-tagged PDEδ (40?nM) in 200?μL PBS-buffer (containing 0.05% CHAPS, 1% DMSO), keeping the concentration of fluorescein-labelled atorvastatin, PDEδ and DMSO constant. For Kd?measurements using isothermal titration calorimetry, PDEδ protein (280?μM) is titrated to small molecule (30?μM) in Tris/HCl buffer (temperature 25°C). In the Tm shift assays, protein melting points are detected by circular dichroism spectroscopy in the presence of small molecules.
Molecular Weight 603.75
Formula C40H37N5O
CAS No. 1440898-61-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (154 mM)

DMSO: 93 mg/mL (154 mM)

TargetMolReferences and Literature

1. Zimmermann G, et al. Nature. 2013, 497(7451), 638-642.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Ovarian Cancer Compound Library Anti-Cancer Compound Library PPI Inhibitor Library Anti-Liver Cancer Compound Library Anti-Obesity Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Anti-Colorectal Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Deltarasin 1440898-61-2 GPCR/G Protein MAPK Metabolism Ras PDE Phosphodiesterase (PDE) inhibit Inhibitor inhibitor

 

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