Deltarasin _Ras 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDeltarasinCat. No.: HY-15747CAS No.: 1440898-61-2分式: CHNO分量: 603.75作靶點(diǎn): Ras; Phosphodiesterase (PDE)作通路: GPCR/G Protein; Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DM

2、SO : 42 mg/mL (69.57 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6563 mL 8.2816 mL 16.5631 mL5 mM 0.3313 mL 1.6563 mL 3.3126 mL10 mM 0.1656 mL 0.8282 mL 1.6563 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) Deltarasin is prepared in PBS2.BIOLOG

3、ICAL ACTIVITY物活性 Deltarasin種 KRAS-PDE 相互作的抑制劑，能夠與 PDE 結(jié)合，Kd 值為 38 nM。IC50 & Target Kd: 38 nM (PDE)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 In liver cells, deltarasin inhibits the interaction of RAS with PDE with Kd of 41 nM. Inhibition of PDE-KRASinteraction by deltarasin suppresses pro

4、liferation of human pancreatic ductal adenocarcinoma cells that aredependent on oncogenic KRAS 1.體內(nèi)研究 Deltarasin (10 mg/kg, i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous humanPanc-Tu-I tumour cell xenografts 1.PROTOCOLKinase Assay 1 Kd values are measured by fluorescenc

5、e polarization measurements. For direct titrations, increasingamounts of PDE are added to a solution containing 50-100 nM labelled small molecule in 200 L PBSbuffer. For displacement titrations, increasing amounts of the small molecules in DMSO are directly added tofluorescein-labelled atorvastatin

6、(24 nM) and His6-tagged PDE (40 nM) in 200 L PBS-buffer (containing0.05% CHAPS, 1% DMSO), keeping the concentration of fluorescein-labelled atorvastatin, PDE and DMSOconstant. For Kd measurements using isothermal titration calorimetry, PDE protein (280 M) is titrated tosmall molecule (30 M) in Tris/

7、HCl buffer (temperature 25C). In the Tm shift assays, protein melting pointsare 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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Nat Commun. 2017 May 16;8:15205.Se

8、e more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDE interaction impairs oncogenic KRAS signalling. Nature. 2013 May30;497(7451):638-42.2. Agalioti T, et al. Mutant KRAS promotes malignant pleural effusion formation. Nat Commun. 2017 May 16;8:15205. doi:10.1038/ncomms15205.McePdfHeightCaution: Product has not been fully validated for medical applicati