Bcr-Abl

Bcr-Abl inhibitors target the constitutively active fusion tyrosine kinase encoded by the Philadelphia chromosome. The translocation joins the breakpoint cluster region (BCR) gene to the Abelson tyrosine kinase gene (ABL1) on chromosome 22. Expression of the P210 form of Bcr-Abl in mouse bone marrow cells induced a disease resembling chronic myelogenous leukemia (CML) in 1990. In 1996 imatinib (CGP 57148), listed here as the base and as imatinib mesylate, was reported to inhibit Abl and Bcr-Abl-positive cell growth. Dasatinib, described in 2004, also inhibits Src family kinases and blocks many imatinib-resistant Abl mutants. Nilotinib and bafetinib are further Abl inhibitors, and ponatinib also inhibits the T315I gatekeeper mutant.

Items 76-86 of 86

  • DosatiLink-2
    Cat. No.
    A33634

    DosatiLink-2

    DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor that functions by selectively inhibiting the kinase activity of the ABL protein. This compound demonstrates significant biological activity against ABL-driven malignancies, making it a valuable tool for research in cancer biology and therapeutic development. It is particularly useful in studies assessing the role of ABL in oncogenesis and resistance mechanisms in cancer treatment.

    Out of stock

    All 3 sizes
  • c-ABL-IN-2
    Cat. No.
    A33643

    c-ABL-IN-2

    c-ABL-IN-2 is a selective inhibitor of c-Abl, a tyrosine kinase implicated in various pathologies, particularly cancer. This compound demonstrates significant potential for investigating neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD). Additionally, c-ABL-IN-2 features an alkyne group, enabling it to function as a click chemistry reagent that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • BCR-ABL-IN-6
    Cat. No.
    A33644

    BCR-ABL-IN-6

    BCR-ABL-IN-6 is a selective Bcr-Abl kinase inhibitor targeting the Bcr-Abl fusion protein, with IC50 values of 4.6 nM for Bcr-AblWT and 227 nM for Bcr-AblT315I. It effectively inhibits Bcr-Abl kinase activity within cells, demonstrating an EC50 of 14.6 nM. As an imatinib derivative, BCR-ABL-IN-6 is applicable in research related to chronic myelogenous leukemia. Additionally, this compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, thus serving as a useful click chemistry reagent in various experimental contexts.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • c-ABL-IN-4
    Cat. No.
    A33645

    c-ABL-IN-4

    c-ABL-IN-4 is a potent inhibitor of the c-Abl tyrosine kinase, a critical target in the treatment of various malignancies and neurodegenerative disorders. Inhibition of c-Abl has been associated with potential therapeutic effects in conditions such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD), as well as in cancer research. This compound facilitates the exploration of c-Abl’s role in disease pathology and therapeutic intervention strategies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • BCR-ABL-IN-4
    Cat. No.
    A33646

    BCR-ABL-IN-4

    BCR-ABL-IN-4 is a potent inhibitor of the BCR-ABL oncogene, exhibiting significant anticancer activity. It effectively suppresses the proliferation of cancer cells, demonstrating IC50 values of 0.67 nM in K562 cells and 16 nM in BCR-ABL T315I transfected Ba/F3 cells. This compound is valuable for research applications focused on targeted cancer therapies and understanding resistance mechanisms in BCR-ABL positive malignancies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • GNF-6
    Cat. No.
    A33647

    GNF-6

    GNF-6 is a potent inhibitor of the BCR-ABL-T315I mutation, acting primarily as an ATP-competitive inhibitor. It demonstrates inhibitory activity with IC50 values of 0.25 μM for c-ABL-T334I, 0.09 μM for BCR-ABL, and 0.590 μM for the BCR-ABL-T315I variant. By disrupting the assembly of the hydrophobic spine, GNF-6 stabilizes the kinase in an inactive 'DFG-out' conformation, making it a valuable tool for research on resistance mechanisms in chronic myeloid leukemia (CML) and targeted therapeutic strategies.

    Out of stock

    All 3 sizes
  • PonatiLink-1-24
    Cat. No.
    A33650

    PonatiLink-1-24

    PonatiLink-1-24 is an inhibitor of the Abelson murine leukemia virus (ABL) enzyme. This compound demonstrates significant biological activity by selectively inhibiting ABL kinase activity, which is vital in various malignancies. It is particularly useful in studying cancer cell signaling pathways and the development of targeted therapies for ABL-related disorders.

    Out of stock

    All 3 sizes
  • AP-24226
    Cat. No.
    A33652

    AP-24226

    AP-24226 is a selective inhibitor of the non-receptor tyrosine kinases Src and ABL. It exhibits significant activity in hindering cell proliferation and survival in various cancer cell lines, making it a valuable tool for cancer research. Its specificity for Src/ABL pathways allows for detailed investigations into their roles in oncogenic processes and therapeutic responses.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Tyrosine kinase-IN-9
    Cat. No.
    A33653

    Tyrosine kinase-IN-9

    Tyrosine kinase-IN-9 is a potent inhibitor of the c-Abl tyrosine kinase. This compound demonstrates significant biological activity in modulating signaling pathways associated with neurodegenerative diseases such as Alzheimer’s and Parkinson’s disease. It serves as a valuable research tool for investigating the roles of c-Abl in cellular processes related to these conditions.

    10 mg
    $850.00
    25 mg
    $1,570.00
    All 2 sizes
  • BCR-ABL kinase-IN-3
    Cat. No.
    A33654

    BCR-ABL kinase-IN-3

    BCR-ABL kinase-IN-3 is a potent inhibitor of the BCR-ABL fusion protein, a critical driver in the pathology of acute myeloid leukemia (AML). This compound exhibits significant biological activity in inhibiting the kinase activity, making it a valuable tool for research into therapeutic strategies targeting BCR-ABL-related malignancies. Its application spans the investigation of molecular mechanisms underlying leukemia and the development of innovative treatments for improved patient outcomes.

    25 mg
    $1,360.00
    50 mg
    $1,790.00
    All 3 sizes
  • BCR-ABL-IN-11
    Cat. No.
    A33658

    BCR-ABL-IN-11

    BCR-ABL-IN-11 is a selective BCR-ABL inhibitor that exhibits significant anticancer activity in chronic myelogenous leukemia (CML) models. With an IC50 value of 129.61 μM in K562 cells, BCR-ABL-IN-11 is a useful tool for studying the molecular mechanisms underlying CML and for evaluating potential therapeutic strategies targeting this oncogenic fusion protein. Its efficacy makes it suitable for research applications focused on leukemia treatment and drug resistance mechanisms.

    Out of stock

    All 3 sizes

Items 76-86 of 86

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