1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

Deltarasin 

Cat. No.: HY-15747 Purity: 95.95%
Handling Instructions

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

For research use only. We do not sell to patients.

Deltarasin Chemical Structure

Deltarasin Chemical Structure

CAS No. : 1440898-61-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 239 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1008 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Deltarasin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

Kd: 38 nM (PDEδ)

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 tumour cell xenografts[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.6563 mL 8.2816 mL 16.5631 mL
5 mM 0.3313 mL 1.6563 mL 3.3126 mL
10 mM 0.1656 mL 0.8282 mL 1.6563 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

603.75

Formula

C₄₀H₃₇N₅O

CAS No.

1440898-61-2

SMILES

C1(C2=CC=C(OC[[email protected]@H](N3C4=CC=CC=C4N=C3C5=CC=CC=C5)C6CCNCC6)C=C2)=NC7=CC=CC=C7N1CC8=CC=CC=C8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 42 mg/mL

Deltarasin is prepared in PBS[2].

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

References

Purity: 95.95%

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Deltarasin
Cat. No.:
HY-15747
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