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    MGCD-265 analog
    MGCD-265 analog

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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 #: V0520
    CAS #: 875337-44-3Purity ≥98%

    Description: MGCD-265 analog (Glesatinib analog) is a potent, orally bioavailable, and ATP-competitive multi-kinase inhibitor with potential antitumor activity. It inhibits c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively. MGCD265 analog has been studied in clinical trials for patients with advanced solid tumors including NSCLC, as a monotherapy and in combination with either docetaxel or erlotinib. In a phase I study, MGCD265 analog was given orally from 24 mg/m2 daily to 235 mg/m2 twice daily uninterrupted to patients with advanced solid malignancy until disease progression.

    References: Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8; J Clin Oncol 28, 2010 (suppl; abstr e13595).

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    Molecular Weight (MW)517.60
    FormulaC26H20FN5O2S2 
    CAS No.875337-44-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 104 mg/mL (200.9 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)

    Chemical Name: N-((3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide

    InChi Key: UFICVEHDQUKCEA-UHFFFAOYSA-N

    InChi Code: InChI=1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35)

    SMILES Code: O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=CN(C)C=N4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=CC=C5

    Synonyms

    MGCD265-analog; Glesatinib-analog; MGCD-265-analog; MGCD 265-analog; 


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    In Vitro

    In vitro activity: MGCD-265 analog is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 analog potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. MGCD-265 analog inhibits cell proliferation both in c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and in non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), with IC50 values of 6 nM–30 nM and 1 μM–3 μM, respectively. In serum starved MKN45 cells, MGCD-265 analog(40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265  analog (6 nM–1 μM) also induces apoptosis in MKN45 cells


    Kinase Assay: MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively. IC50 value:10 nM (VEGFR2), 29 nM(c-Met) 


    Cell Assay: Cells (HCT116, MDA-MB-231, SNU-5, and MKN45 cells) are treated with MGCD-265 analog for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours.

    In VivoIn c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 tumor cells, MGCD-265 analog (20 mg/kg–60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 analog (40 mg/kg) also downregulates genes involved in angiogenesis, including VEGF and IL-8, both in tumor and plasma of mice with U87MG xenograft. MGCD-265 analog also inhibits the plasma level of shed-Met.
    Animal modelMice
    Formulation & Dosage20–60 mg/kg
    References

    J. M. Besterman, M. Fournel, I. Dupont, C. Bonfils, M. Dubay, H. Ste-Croix, C. R. Maroun; MethylGene, Inc., Montreal, QC, Canada, Potent preclinical antitumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib, J Clin Oncol 28, 2010 (suppl; abstr e13595).


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

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