1. GPCR/G Protein Metabolic Enzyme/Protease
  2. Ras Phosphodiesterase (PDE)
  3. Deltarasin hydrochloride

Deltarasin hydrochloride 

Cat. No.: HY-15747A Purity: 99.97%
COA 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. : 1613404-76-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 254 In-stock
Solution
10 mM * 1 mL in DMSO USD 254 In-stock
Solid
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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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Deltarasin hydrochloride:

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Deltarasin hydrochloride

View All Ras Isoform Specific Products:

  • Biological Activity

  • Protocol

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  • References

  • Customer Review

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].

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

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].

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

Molecular Weight

640.22

Appearance

Solid

Formula

C40H38ClN5O

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 52 mg/mL (81.22 mM)

H2O : 50 mg/mL (78.10 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
Purity & Documentation
References
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
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Deltarasin hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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