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    Deltarasin
    Deltarasin

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0784
    CAS #: 1440898-61-2 Purity ≥98%

    Description: Deltarasin (also known as Deltarasin hydrochloride) is a novel, high affinity and potent small molecule inhibitor of KRAS-PDEδ protein-protein interaction with potential antineoplastic activity. It inhibits KRAS-PDEδ interaction with a Kd of 38 nM for binding to purified PDEδ. The KRAS oncogene product is considered a major target in anticancer drug discovery. 5 mM of deltarasin completely inhibited PDEδ-KRAS interaction and released the insolubilized mCitrine-RHEB/KRAS6Q to the endomembrane system. This showed that deltarasin interfered with the binding of KRAS to PDEδ in cells and thereby inhibited its solubilization 

    References: Nature. 2013 May 30;497(7451):638-42.

    Related CAS: 1440898-61-2 (free base); 1440898-82-7 (HCl) 

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    Molecular Weight (MW)603.75
    FormulaC40H37N5O
    CAS No.1440898-61-2 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (165.6 mM) 
    Water:<1 mg/mL
    Ethanol: <1 mg/L
    SMILESC1(C2=CC=C(OC[[email protected]@H](N3C4=CC=CC=C4N=C3C5=CC=CC=C5)C6CCNCC6)C=C2)=NC7=CC=CC=C7N1CC8=CC=CC=C8
    SynonymsDeltarasin hydrochloride; Deltarasin HCl; Deltarasin;

    Chemical Name: 2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole, trihydrochloride

    InChi Key: NCIOVAYUMQEQEU-VKZSUDIWSA-N

    InChi Code: InChI=1S/C40H37N5O.3ClH/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31;;;/h1-22,30,38,41H,23-28H2;3*1H/t38-;;;/m1.../s1


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    In Vitro

    In vitro activity: 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.


    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.


    Cell Assay: Within a minute, 5 mM of deltarasin completely inhibited PDEδ-KRAS interaction and released the insolubilized mCitrine-RHEB/KRAS6Q to the endomembrane system. This showed that deltarasin interfered with the binding of KRAS to PDEδ in cells and thereby inhibited its solubilization.

    In VivoDeltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts.
    Animal modelMice bearing Panc-Tu-I xenografts
    Formulation & DosageDissolved in 10% PLR and 5% DMSO; 10 mg/kg; Administered through i.p.
    ReferencesNature. 2013 May 30;497(7451):638-42.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Deltarasin

    In-cell measurements of the effect of deltarasin on the interaction of RAS with PDEδ and resulting delocalization of KRAS. Nature. 2013 May 30;497(7451):638-42. 
     

    Deltarasin

    Inhibition of PDEδ–KRAS interaction suppresses proliferation and MAPK-signalling in oncogenic KRAS-dependent PDAC cells. Nature. 2013 May 30;497(7451):638-42. 
     

    Deltarasin

    Deltarasin impairs dose-dependent in vivo growth of xenografted pancreatic carcinoma in nude mice. Nature. 2013 May 30;497(7451):638-42. 


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