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.

Bcr-Abl Isoform Specific Products:

Bcr-Abl Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15268
    PP487
    		Inhibitor
    PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research.
    PP487
  • HY-10181G
    Dasatinib (GMP)
    		Inhibitor
    Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values ​​for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50 values ​​of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib (GMP)
  • HY-12083
    PPY-A
    		Inhibitor
    PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML).
    PPY-A
  • HY-101268
    CHMFL-ABL-053
    		Inhibitor
    CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC50 values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively.
    CHMFL-ABL-053
  • 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-10158AR
    Bosutinib hydrate (Standard)
    		Inhibitor
    Bosutinib (Standard) (SKI-606 (Standard)) hydrate is the analytical standard of Bosutinib hydrate (HY-10158A). This product is intended for research and analytical applications. Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50s of 1.2 nM and 1 nM, respectively.
    Bosutinib hydrate (Standard)
  • 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-176269
    VS1150
    		Inhibitor
    VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research.
    VS1150
  • 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 (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.
    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, KDR, 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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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