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

Bcr-Abl

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:

Cat. No. Product Name Effect Purity Chemical Structure
  • 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
  • HY-153582
    ML 2-23
    Degrader
    ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells.
    ML 2-23
  • HY-146697
    IHMT-TRK-284
    Inhibitor
    IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.
    IHMT-TRK-284
  • HY-111874
    SNIPER(ABL)-039
    Inhibitor
    SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively.
    SNIPER(ABL)-039
  • HY-155290
    PonatiLink-1-24
    Inhibitor
    PonatiLink-1-24 is an Abelson murine leukemia (ABL) enzyme inhibitor.
    PonatiLink-1-24
  • HY-W839261
    Tyrosine kinase-IN-9
    Inhibitor
    Tyrosine kinase-IN-9 (Compound B) is the inhibitor for c-Abl. Tyrosine kinase-IN-9 can be used in research of neurodegenerative diseases including Alzheimer’s and Parkinson’s disease.
    Tyrosine kinase-IN-9
  • HY-160174
    BCR-ABL kinase-IN-3
    Inhibitor
    BCR-ABL kinase-IN-3 (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research.
    BCR-ABL kinase-IN-3
  • HY-15666R
    Olverembatinib (Standard)
    Inhibitor
    Olverembatinib (Standard) is the analytical standard of Olverembatinib. This product is intended for research and analytical applications. Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity. Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Olverembatinib (Standard)
  • HY-10158S1
    Bosutinib-13C,d3
    Inhibitor
    Bosutinib-13C,d3 (SKI-606-13C,d3) is 13C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
    Bosutinib-<sup>13</sup>C<sub>,d<sub>3</sub>
  • HY-164469
    CHMFL-48
    Inhibitor
    CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML).
    CHMFL-48
  • HY-10181AR
    Dasatinib hydrochloride (Standard)
    Inhibitor
    Dasatinib (hydrochloride) (Standard) is the analytical standard of Dasatinib (hydrochloride). This product is intended for research and analytical applications. Dasatinib (BMS-354825) hydrochloride 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 hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
    Dasatinib hydrochloride (Standard)
  • HY-50868R
    Bafetinib (Standard)
    Inhibitor
    Bafetinib (Standard) is the analytical standard of Bafetinib. This product is intended for research and analytical applications. Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity.
    Bafetinib (Standard)
  • HY-13072B
    Cenisertib benzoate
    Inhibitor
    Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
    Cenisertib benzoate
  • HY-15463S3
    Imatinib-13C,d3
    Inhibitor
    Imatinib-13C,d3 (STI571-13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-117718R
    AG957 (Standard)
    Inhibitor
    AG957 (Standard) is the analytical standard of AG957. This product is intended for research and analytical applications. AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity.
    AG957 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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