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    A-1331852
    A-1331852

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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 #: V2656
    CAS #: 1430844-80-6Purity ≥98%

    Description: A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases. A-1331852 demonstrated cellular activity 10- to 50-fold more potent than its analog A-1155463 and the previouly reported BCL-XL inhibitor, navitoclax, respectively. Moreover, A-1331852 could selectively disrupt BCL-XL–BIM complexes and induce the apoptosis hallmarks in BCL-XL–dependent Molt-4 cells with median IC50 values in the low nanomolar range but did not affect MEF cells without BAK or BAX 

    References: Sci Transl Med. 2015 Mar 18;7(279):279ra40; Leukemia. 2016 Jun;30(6):1273-81. 


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    Molecular Weight (MW)658.81 
    FormulaC38H38N6O3S 
    CAS No.1430844-80-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (151.8 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)
    SynonymsA-1331852; A 1331852; A1331852


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    In Vitro

    In vitro activity: A-1331852 exhibits remarkable potency both as a single agent and in combination with TKIs in killing primary CD34+ CML cell. Also, It has remarkable potency in inducing apoptosis in these cells at low nanomolar concentrations as early as 1 h post-treatment


    Kinase Assay:


    Cell Assay: Immunoprecipitation of BCL-XL is carried out in K562 cells, exposed to A-1331852 (100 nM) for 0-2 h, and the eluted complexes are immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) are immunoblotted to check the efficiency of the immunoprecipitation. 

    In VivoPrevious animal study found that A-1331852 could demonstrate antitumor efficacy in the Molt-4 xenograft model, such as tumor regressions as a single agent. In addition, in the NCI-H1963.FP5 xenograft model of SCLC, it was found that A-1331852 combined with venetoclax was able to recapitulate the efficacy of navitoclax  
    Animal modelSCID and SCID-bg mice 
    Formulation & DosageFormulated in 60% Phosal 50 PG, 27.5 % PEG 400, 10% ethanol, and 2.5% DMSO; 25 mg/kg; Oral gavage
    References

    Sci Transl Med. 2015 Mar 18;7(279):279ra40; Leukemia. 2016 Jun;30(6):1273-81.  


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

    A-1331852

    BCL-XL is a critical survival factor and regulates TKI-induced apoptosis in CML cell lines. Leukemia. 2016 Jun;30(6):1273-81.



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