My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    IXAZOMIB (MLN2238)
    IXAZOMIB (MLN2238)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0688
    CAS #: 1072833-77-2Purity ≥98%

    Description: Ixazomib (formerly also known as MLN-2238) is a novel, potent, selective and reversible proteasome inhibitor (PI) with potential antineoplastic activity. It inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, it also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.  MNL-2238 is the biologically active form of MLN9708 with an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI-Ly10 and PHTX22L models.

    References: Cancer Res. 2010 Mar 1;70(5):1970-80; Clin Cancer Res. 2011 Dec 1;17(23):7313-23.

    Related CAS #: 1239908-20-3 (citrate)   1072833-77-2 (free)   1201902-80-8    

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)361.03
    FormulaC14H19BCl2N2O4
    CAS No.1072833-77-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 72 mg/mL (199.4 mM)
    Water: <1 mg/mL
    Ethanol: 9 mg/mL (24.9 mM)
    Solubility (In vivo)0.5% hydroxyethyl cellulose: 30 mg/mL
    SynonymsMLN-2238; MLN2238; IXAZOMIB; MLN 2238; Trade name: Ninlaro.

    IUPAC/Chemical Name: (R)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic acid

    InChi Key: MXAYKZJJDUDWDS-LBPRGKRZSA-N

    InChi Code: InChI=1S/C14H19BCl2N2O4/c1-8(2)5-12(15(22)23)19-13(20)7-18-14(21)10-6-9(16)3-4-11(10)17/h3-4,6,8,12,22-23H,5,7H2,1-2H3,(H,18,21)(H,19,20)/t12-/m0/s1

    SMILES Code: CC(C)C[[email protected]@H](B(O)O)NC(CNC(C1=CC(Cl)=CC=C1Cl)=O)=O


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: At higher concentrations, MLN2238 also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31nM and 3.5uM, respectively. MLN2238 inhibits Calu-6 cell with IC50 of 9.7 nM. MLN2238 is a selective, potent, and reversible inhibitor of the proteasome in tumor cells. MLN2238 shows time-dependent reversible proteasome inhibition. Both MLN2238 and Bortezomib shows time-dependent reversible proteasome inhibition; however, the proteasome dissociation half-life for MLN2238 is determined to be ∼6-fold faster than that of Bortezomib (18 and 110 minutes, respectively). MLN2238 dissociates more rapidly from the proteasome than Bortezomib, consistent with faster recovery of proteasome activity observed in the Proteasome-Glo assay. MLN2238 has a greater overall tumor pharmacodynamic effect than Bortezomib as assessed by 20S inhibition. MLN2238 is the biologically active form of MLN9708.


    Kinase Assay: Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument.


    Cell Assay: Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37 °C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37 °C and then washed thrice in medium to remove the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37 °C, after which the medium is removed and replaced with fresh medium.

    In VivoMLN2238 induces a greater pharmacodynamic response than Bortezomib in xenograft tumors. MLN2238 shows greater maximum and sustained tumor proteasome inhibition compared with Bortezomib in xenograft models. These results confirm that the improved tumor exposure seen with MLN2238 translates into an improved tumor pharmacodynamic response both at the level of and downstream from the proteasome. MLN2238 shows antitumor activity in the CWR22 xenograft model. MLN2238 shows greater tumor pharmacodynamic responses in WSU-DLCL2 xenografts compared with Bortezomib. Similarly, Bortezomib treatment only led to a minor increase in GADD34 levels in WSU-DLCL2 xenograft tumors, whereas MLN2238 strongly induces its expression. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with Bortezomib in both OCI-Ly10 and PHTX22L models
    Animal modelCB-17 SCID mice are subcutaneously inoculated with MM.1S cells
    Formulation & DosageDissolved in 5% 2-hydroxypropyl-β-cyclodextrin; 11 mg/kg; i.v. injection
    References

    Cancer Res. 2010 Mar 1;70(5):1970-80; Clin Cancer Res. 2011 Dec 1;17(23):7313-23.



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

     

    IXAZOMIB (MLN2238)

    Proteasome inhibition and antitumor activity of bortezomib and MLN2238 in tumor xenograft models of activated B-cell diffuse large B-cell lymphoma. Clin Cancer Res. 2011 Dec 1;17(23):7313-23. 
     

    IXAZOMIB (MLN2238)

    Osteolytic bone disease in the iMycCα/Bcl-XL GEM model of de novo PCM. Clin Cancer Res. 2011 Dec 1;17(23):7313-23. 
     

    IXAZOMIB (MLN2238)

    Antitumor activity of bortezomib and MLN2238 in the disseminated mouse model of DP54-Luc iMycCα/Bcl-XL PCM. Clin Cancer Res. 2011 Dec 1;17(23):7313-23. 

    IXAZOMIB (MLN2238)

    IXAZOMIB (MLN2238)

    IXAZOMIB (MLN2238)



    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?