Deltarasin NEW
| Price | $38 | $75 | $135 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Deltarasin | CAS No.: 1440898-61-2 |
| Purity: 99.06% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Deltarasin |
| Description | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 93 mg/mL (154 mM) DMSO : 93 mg/mL (154 mM) |
| Keywords | Phosphodiesterase (PDE) | inhibit | Deltarasin | Inhibitor | Ras |
| Inhibitors Related | Theophylline monohydrate | Acefylline | MRTX1133 | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $0.00/5mg |
VIP6Y
|
Shaanxi Dideu Medichem Co. Ltd
|
2019-12-30 | |
| $1.00/1KG |
VIP7Y
|
Career Henan Chemical Co
|
2018-08-21 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY