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-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-41940
    Dasatinib intermediate-1
    		Control
    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-10158R
    Bosutinib (Standard)
    		Inhibitor
    Bosutinib (Standard) is the analytical standard of Bosutinib. This product is intended for research and analytical applications. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
    Bosutinib (Standard)
  • HY-132549S
    Nilotinib-d3
    		Inhibitor
    Nilotinib-d3 is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2].
    Nilotinib-d<sub>3</sub>
  • HY-123486
    HS-438
    		Inhibitor
    HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML).
    HS-438
  • 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-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-169608
    BCR-ABL-IN-11
    		Inhibitor
    BCR-ABL-IN-11 (Compound 2) is a BCR-ABL inhibitor. BCR-ABL-IN-11 shows anticancer activity against chronic myelogenous leukemia (CML) (IC50 of 129.61 μM for K562 cells).
    BCR-ABL-IN-11
  • HY-18817
    AFG210
    		Inhibitor
    AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.
    AFG210
  • HY-12047R
    Ponatinib (Standard)
    		Inhibitor
    Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. 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/KDR/Flk-1, FGFR1, and Src, respectively.
    Ponatinib (Standard)
  • HY-15493
    AN-019
    		Inhibitor
    AN-019 is a Bcr-Abl kinase inhibitor. AN-019 has antitumor activity.
    AN-019
  • HY-160174A
    BCR-ABL kinase-IN-3 (dihydrocholide)
    		Inhibitor
    BCR-ABL kinase-IN-3 (dihydrocholide) (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 (dihydrocholide)
  • HY-164393
    ON044580
    		Inhibitor
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.
    ON044580
  • HY-W700620
    Hydroxymethyl dasatinib
    		Inhibitor 99.92%
    Hydroxymethyl dasatinib (M24), a benzylhydroxy metabolite of Dasatinib (HY-10181), exhibits an IC50 of 46.7nM in K562 CML cells.
    Hydroxymethyl dasatinib
  • HY-15463R
    Imatinib (Standard)
    		Inhibitor
    Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. 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 (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)
  • HY-10159AR
    Nilotinib (monohydrochloride monohydrate) (Standard)
    		Inhibitor
    Nilotinib (monohydrochloride monohydrate) (Standard) is the analytical standard of Nilotinib (monohydrochloride monohydrate). This product is intended for research and analytical applications. Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
    Nilotinib (monohydrochloride monohydrate) (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity