Deltarasin NEW
| Price | $38 | $75 | $135 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-11 |
Product Details
| Product Name: Deltarasin | CAS No.: 1440898-61-2 |
| Purity: 99.06% | Supply Ability: 10g |
| Release date: 2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | Deltarasin |
| 描述 | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 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] |
| 體內(nèi)活性 | 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. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 93 mg/mL (154 mM) DMSO : 93 mg/mL (154 mM) |
| 關(guān)鍵字 | Phosphodiesterase (PDE) | inhibit | Deltarasin | Inhibitor | Ras |
| 相關(guān)產(chǎn)品 | Theophylline monohydrate | Acefylline | MRTX1133 | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| 相關(guān)庫(kù) | 抗結(jié)直腸癌化合物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 抗癌化合物庫(kù) | 抗肝癌化合物庫(kù) |
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.
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