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

Deltarasin hydrochloride 

Cat. No.: HY-15747A
Handling Instructions

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

For research use only. We do not sell to patients.
Deltarasin hydrochloride Chemical Structure

Deltarasin hydrochloride Chemical Structure

CAS No. : 1440898-82-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 254 In-stock
5 mg USD 180 In-stock
10 mg USD 252 In-stock
50 mg USD 1008 In-stock
100 mg USD 1800 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Deltarasin hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction 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 1.5620 mL 7.8098 mL 15.6196 mL
5 mM 0.3124 mL 1.5620 mL 3.1239 mL
10 mM 0.1562 mL 0.7810 mL 1.5620 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

640.22

Formula

C₄₀H₃₈ClN₅O

CAS No.

1440898-82-7

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: ≥ 52 mg/mL

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

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Product Name:
Deltarasin hydrochloride
Cat. No.:
HY-15747A
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