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    OSI-930
    OSI-930

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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 #: V0509
    CAS #: 728033-96-3Purity ≥98%

    Description: OSI-930 is an orally bioavailable, potent and selective inhibitor of multi-kinase (Kit, KDR and CSF-1R) with potential antineoplastic activity. It inhibits Kit, KDR and CSF-1R with IC50s of 80 nM, 9 nM and 15 nM, respectively; It is also potent against Flt-1, c-Raf and Lck but shows low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 is a thiophene-derived tyrosine kinase inhibitor that shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy.

    References: Cancer Res. 2006 Jan 15;66(2):1015-24; Drug Metab Dispos. 2011 Feb;39(2):345-50.

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    Molecular Weight (MW)443.44
    FormulaC22H16F3N3O2S
    CAS No.728033-96-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (200.7 mM)
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (6.76mM)
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 5 mg/kg
    Synonyms

    Synonym: OSI-930; OSI 930; OSI930.

    Chemical Name: 3-((quinolin-4-ylmethyl)amino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide

    InChi Key: FGTCROZDHDSNIO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C22H16F3N3O2S/c23-22(24,25)30-16-7-5-15(6-8-16)28-21(29)20-19(10-12-31-20)27-13-14-9-11-26-18-4-2-1-3-17(14)18/h1-12,27H,13H2,(H,28,29)

    SMILES Code: O=C(C1=C(NCC2=CC=NC3=CC=CC=C23)C=CS1)NC4=CC=C(OC(F)(F)F)C=C4


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    In Vitro

    In vitro activity: OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode.


    Kinase Assay: Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at −80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit.


    Cell Assay: For assays of cell proliferation and apoptosis, cells are seeded into 96-well plates and incubated for 2 to 3 days in the presence of OSI-930 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of the intracellular ATP content using CellTiterGlo. Induction of caspase-dependent apoptosis by OSI-930 is quantitated by an enzymatic caspase 3/7 assay. Inhibition of angiogenesis by OSI-930 is monitored using the rat aortic ring endothelial sprout outgrowth assay. Sections of aorta are prepared from CO2-euthanized male rats and cultured in vitro in a collagen matrix in the presence or absence of OSI-930. The collagen matrix is prepared from type 1 rat tail collagen solubilized in 0.1% acetic acid at 3 mg/mL, which is combined with 0.125 volume collagen buffer (0.05 N NaOH, 200 mM HEPES, 260 mM NaHCO3), 0.125 volume of medium 199, 0.0125 volume of 1 M NaOH, and 1% GlutaMax. Aortic rings are embedded in 0.4 mL of this matrix in six-well plates, to which 0.5 mL endothelial basal medium and the appropriate amount of OSI-930 is added; the rings are then incubated for 10 days and the resultant angiogenic sprout outgrowth is digitally quantitated from images by measurement of the sprout-containing area within a series of concentric rings around the aortic tissue area.

    In VivoOSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models.
    Animal modelCD1 nu/nu mice bearing HMC-1, NCI-SNU-5, COLO-205 and U251 cells
    Formulation & Dosage Dissolved in either Labrafil M 1944 CS or polyethylene glycol (PEG)-400/water (50:50); ~200 mg/kg; p.o.
    References

    Cancer Res. 2006 Jan 15;66(2):1015-24; Drug Metab Dispos. 2011 Feb;39(2):345-50.


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

    OSI-930

    Inhibition of endothelial cell function by OSI-930 in vitro.Cancer Res. 2006 Jan 15;66(2):1015-24.

    OSI-930

    Pharmacokinetic/pharmacodynamic relationship of OSI-930 in the HMC-1 tumor xenograft model and correlation with antitumor activity. Cancer Res. 2006 Jan 15;66(2):1015-24.

    OSI-930

    Pharmacodynamic effects of OSI-930 and correlation with antitumor activity. Cancer Res. 2006 Jan 15;66(2):1015-24.


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