2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Bcr-Abl

Bcr-Abl

Bcr-Abl

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Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome. This abnormality is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 and the break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been implicated in the pathogenesis of CML. Compounds have been developed to selectively inhibit the tyrosine kinase.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-155289
    DosatiLink-2
    		Inhibitor
    DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor.
    DosatiLink-2
  • HY-128397
    CpCDPK1/TgCDPK1-IN-1
    		Inhibitor
    CpCDPK1/TgCDPK1-IN-1 (compound 7p) is a potent CpCDPK1/TgCDPK1 dual inhibitor (IC50: 10 nM and 5.0 nM respectively). CpCDPK1/TgCDPK1-IN-1 also inhibits Abl and Src (IC50: 75 nM and 65 nM respectively). CpCDPK1/TgCDPK1-IN-1 can be used for research of toxoplasmosis.
    CpCDPK1/TgCDPK1-IN-1
  • HY-162952
    cSRC/BCR-ABL1-IN-1
    		Inhibitor
    cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor.
    cSRC/BCR-ABL1-IN-1
  • HY-162489
    Tyrosine kinase-IN-8
    		Inhibitor
    Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia.
    Tyrosine kinase-IN-8
  • HY-100314
    BCR-ABL-IN-1
    		Inhibitor
    BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
    BCR-ABL-IN-1
  • HY-15728S
    Radotinib-d6
    Radotinib-d6 is deuterium labeled Radotinib.
    Radotinib-d<sub>6</sub>
  • HY-169230
    BCR-ABL-IN-9
    		Inhibitor
    BCR-ABL-IN-9 (Compound B1) is a BCR-ABL inhibitor that achieves sustained BCR-ABL suppression by forming stable covalent bonds with the ABL kinase. BCR-ABL-IN-9 is also effective in inhibiting the activity of the ABL kinase (IC50 = 1.2 nM). BCR-ABL-IN-9 possesses anticancer activity.
    BCR-ABL-IN-9
  • HY-14979
    ML786
    		Inhibitor
    ML786 is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 also inhibits Abl-1, DDR2, EPHA2, VEGFR2/KDR/Flk-1, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.
    ML786
  • HY-146527
    c-ABL-IN-2
    		Inhibitor
    c-ABL-IN-2 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-2 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2020260871A1, compound 25). c-ABL-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    c-ABL-IN-2
  • HY-150569
    BCR-ABL-IN-6
    		Inhibitor
    BCR-ABL-IN-6 (9h) is a selective Bcr-Abl kinase inhibitor with IC50s of 4.6 and 227 nM for Bcr-AblWT and Bcr-AblT3151 respectively. BCR-ABL-IN-6 inhibits Bcr-Abl kinase with strong affinity inside the cells with an EC50 of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia. BCR-ABL-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    BCR-ABL-IN-6
  • HY-126143
    CHMFL-ABL-039
    		Inhibitor
    CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.
    CHMFL-ABL-039
  • HY-118084
    LS-104
    		Inhibitor
    LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies.
    LS-104
  • HY-146530
    c-ABL-IN-4
    		Inhibitor
    c-ABL-IN-4 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-4 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 54).
    c-ABL-IN-4
  • HY-50946R
    Imatinib (Mesylate) (Standard)
    		Inhibitor
    Imatinib (Mesylate) (Standard) is the analytical standard of Imatinib (Mesylate). This product is intended for research and analytical applications. Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
    Imatinib (Mesylate) (Standard)
  • HY-142922
    BCR-ABL-IN-4
    		Inhibitor
    BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11).
    BCR-ABL-IN-4
  • HY-160478
    GNF-6
    		Inhibitor
    GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation.
    GNF-6
  • HY-156102
    c-ABL-IN-5
    c-ABL-IN-5 is a selective c-Abl inhibitor with neuroprotective effects. c-ABL-IN-5 has blood-brain barrier penetrability, metabolic stability and good pharmacokinetic properties. When c-ABL-IN-5 is labeled with [18F] (compound [18F]3), it can be used as a tracer to evaluate disease-modifying efficacy by complementary positron emission tomography (PET). c-ABL-IN-5 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD).
    c-ABL-IN-5
  • HY-10159S1
    Nilotinib-13C,d3
    		Inhibitor
    Nilotinib-13C,d3 is a deuterated labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-10181BR
    Dasatinib (monohydrate) (Standard)
    		Inhibitor
    Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
    Dasatinib (monohydrate) (Standard)
  • HY-163189
    c-ABL-IN-6
    		Inhibitor
    c-ABL-IN-6 (compound A6) is a c-ABL inhibitor with IC50 value of 16.6 nM. c-ABL-IN-6 displays higher neuroprotective effects against SH-SY5Y cell death induced by MPP+ (HY-W008719). c-ABL-IN-6 can be used for the research of neurodegenerative disorder.
    c-ABL-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity