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    CB-5083
    CB-5083

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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 #: V0181
    CAS #: 1542705-92-9Purity ≥98%

    Description: CB-5083 is a novel, potent, selective, first in class and orally bioavailable p97 AAA ATPase inhibitor with potential anticancer activity. It inhibits p97 AAA ATPase with an IC50 of 11 nM. CB-5083 disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models. CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer.

    References: J Med Chem. 2015 Dec 24;58(24):9480-97.

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    Molecular Weight (MW)413.47
    FormulaC24H23N5O2 
    CAS No.1542705-92-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (200.7 mM)
    Water: <1 mg/mL
    Ethanol: 13 mg/mL (31.4 mM)
    Solubility (In vivo)0.5% CMC Na+5% Tween 80: 30mg/mL 
    Other info

    Synonym: CB5083; CB-5083; CB 5083.

    Chemical Name: 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide

    InChi Key: RDALZZCKQFLGJP-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28)

    SMILES Code: O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N.


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    In Vitro

    In vitro activity: In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM.


    Kinase Assay: Compounds are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution series with duplicate of each compound concentration point. In 5 μL total volume, 20 nM p97 hexameric enzyme and 20 μM ATP are added to start the reaction. The plate is sealed and incubated at 37 °C for 15 min after mixing thoroughly in an orbital shaker. Compound dilution, ATP and enzymes addition are conducted with automated liquid handling using the Freedom Evo. ADP Glo reagents 1 and 2 are added according to the manufacturer’s protocol. The luminescence is measured by Envision plate reader as the end point of the reaction. The IC50 of each compound is derived by fitting the luminescence values to a four-parameter sigmoidal curve.


    Cell Assay: A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability. Luminescence values are fit to a four-parameter sigmoidal curve to determine IC50 concentrations.

    In VivoIn mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition.
    Animal modelNu/Nu nude female mice bearing human HCT 116 colon tumor xenografts
    Formulation & DosageSuspended in 0.5% methylcellulose in water; 75 mg/kg, qd; oral administration
    References

    J Med Chem. 2015 Dec 24;58(24):9480-97.


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

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