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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101489
    GZD856
    Inhibitor
    GZD856 formic is a potent and orally active PDGFRα 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
  • HY-152036
    SIAIS100
    Degrader
    SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML).
    SIAIS100
  • HY-111873
    SNIPER(ABL)-019
    Inhibitor
    SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM.
    SNIPER(ABL)-019
  • HY-111859
    SNIPER(ABL)-058
    Inhibitor
    SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.
    SNIPER(ABL)-058
  • HY-111854
    SNIPER(ABL)-015
    Inhibitor
    SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM .
    SNIPER(ABL)-015
  • HY-111851
    SNIPER(ABL)-049
    Inhibitor
    SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM.
    SNIPER(ABL)-049
  • HY-139730
    c-ABL-IN-1
    Inhibitor
    c-ABL-IN-1 is a novel selective c-Abl inhibitor that prevents neurodegeneration in parkinson’s disease.
    c-ABL-IN-1
  • HY-157497
    DA5-HTL
    Inhibitor
    DA5-HTL is a compound combined dasatinib with HaloTag system efficiently inhibits the growth of the cancer cells with GI50 of 1.923 nM.
    DA5-HTL
  • HY-10363
    AP 24149
    Inhibitor
    AP 24149 is a potent Src-Abl dual inhibitor with IC50 values of 9.1, 3.6 nM for Src and Abl, respectively.
    AP 24149
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity