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-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-12047S
    Ponatinib-d8
    		Inhibitor 99.91%
    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-10181R
    Dasatinib (Standard)
    		Inhibitor
    Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. 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 (Standard)
  • 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-10159C
    Nilotinib hydrochloride dihydrate
    		Inhibitor 99.89%
    Nilotinib (AMN107) hydrochloride dihydrate is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia.
    Nilotinib hydrochloride dihydrate
  • HY-10159B
    Nilotinib hydrochloride
    		Inhibitor
    Nilotinib (AMN107) hydrochloride is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia.
    Nilotinib hydrochloride
  • HY-101489
    GZD856
    		Inhibitor
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
    GZD856
  • HY-136526
    BCR-ABL-IN-3
    		Inhibitor
    BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-AblT3151. BCR-ABL-IN-3 has anti-cancer activity.
    BCR-ABL-IN-3
  • HY-119370
    CHMFL-ABL-121
    		Inhibitor
    CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
    CHMFL-ABL-121
  • HY-101034
    CHMFL-ABL/KIT-155
    		Inhibitor
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
    CHMFL-ABL/KIT-155
  • HY-111871
    SNIPER(ABL)-033
    		Inhibitor
    SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM (ABL inhibitor: HY-15814; ABL inhibitor activity control: HY-131178; E3 ligase ligand: HY-128808; linker: HY-130500; E3 ligase ligand + linker: HY-128819).
    SNIPER(ABL)-033
  • HY-108704
    CT-721
    		Inhibitor
    CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities. CT-721 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CT-721
  • HY-112314
    AZD0424
    		Inhibitor
    AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
    AZD0424
  • HY-111858
    SNIPER(ABL)-050
    		Inhibitor
    SNIPER(ABL)-050, conjugating Imatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
    SNIPER(ABL)-050
  • HY-111861
    SNIPER(ABL)-024
    		Inhibitor
    SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
    SNIPER(ABL)-024
  • HY-10058
    AT9283 lactic acid
    		Inhibitor
    AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo.
    AT9283 lactic acid
  • HY-111862
    SNIPER(ABL)-044
    		Inhibitor
    SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.
    SNIPER(ABL)-044
  • HY-111860
    SNIPER(ABL)-013
    		Inhibitor
    SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 20 μM.
    SNIPER(ABL)-013
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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