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-131178
    HG-7-85-01-NH2
    		98.05%
    HG-7-85-01-NH2 is the HG-7-85-01 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
    HG-7-85-01-NH2
  • HY-10159R
    Nilotinib (Standard)
    		Inhibitor
    Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib (Standard)
  • HY-12338
    ON 146040
    		Inhibitor
    ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
    ON 146040
  • HY-111872
    SNIPER(ABL)-020
    		Inhibitor 99.79%
    SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
    SNIPER(ABL)-020
  • HY-156148
    BCR-ABL-IN-8
    		Inhibitor
    BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group.
    BCR-ABL-IN-8
  • HY-123390
    DB07107
    		Inhibitor
    DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
    DB07107
  • HY-P1785
    Abl Cytosolic Substrate
    		99.60%
    Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ). Abl Protein Tyrosine Kinase (AbI) is a truncated form of the v-AbI Protein Tyrosine Kinase, a partner in the Gag-Abl fusion protein of the Abelson murine leukemia virus.
    Abl Cytosolic Substrate
  • 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-47026
    Protein kinase inhibitor 6
    		Inhibitor 99.04%
    Protein kinase inhibitor 6 is a protein kinase inhibitor.
    Protein kinase inhibitor 6
  • HY-130297
    PROTAC BCR-ABL1 ligand 1
    		Inhibitor 99.17%
    PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
    PROTAC BCR-ABL1 ligand 1
  • HY-15463S2
    Imatinib-d3 hydrochloride
    Imatinib-d3 (hydrochloride) is the deuterium 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-d<sub>3</sub> hydrochloride
  • HY-10158S
    Bosutinib-d8
    		Inhibitor ≥99.0%
    Bosutinib-d8 is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.
    Bosutinib-d<sub>8</sub>
  • 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 an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
    Imatinib Mesylate (Standard)
  • HY-153008
    BCR-ABL-IN-7
    		Inhibitor 99.66%
    BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research.
    BCR-ABL-IN-7
  • HY-12047S
    Ponatinib-d8
    		Inhibitor 99.16%
    Ponatinib-d8 (AP24534-d8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
    Ponatinib-d<sub>8</sub>
  • HY-120508
    Pivanex
    		Inhibitor
    Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.
    Pivanex
  • HY-41940
    Dasatinib intermediate-1
    		Control ≥98.0%
    Dasatinib intermediate-1 is an intermediate in the synthesis of Dasatinib (HY-10181). Dasatinib Is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity.
    Dasatinib intermediate-1
  • HY-10181S1
    Dasatinib-d4
    		Inhibitor
    Dasatinib-d4 (BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) 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 inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib-d<sub>4</sub>
  • HY-13072R
    Cenisertib (Standard)
    		Inhibitor
    Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
    Cenisertib (Standard)
  • HY-104010R
    Asciminib (Standard)
    		Inhibitor
    Asciminib (Standard) is the analytical standard of Asciminib. This product is intended for research and analytical applications. Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
    Asciminib (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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