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  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. Nom du produit Effet Pureté Chemical Structure
  • HY-E70639
    ABL1 Q252H Recombinant Human Active Protein Kinase
    The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 Q252H Recombinant Human Active Protein Kinase is a recombinant ABL1 Q252H protein that can be used to study ABL1 Q252H-related functions.
    ABL1 Q252H Recombinant Human Active Protein Kinase
  • HY-171184
    EAPB0503
    		Inhibitor
    EAPB0503 is a quinoline compound with anti-tumor activity, showing strong cytotoxicity against melanoma cells in vitro (IC50=200 nM). EAPB0503 can induce specific cell cycle arrest in mitosis of CML cells and directly activate apoptosis, leading to an increase in the G0 cell population, disruption of mitochondrial membrane potential, PARP cleavage, and DNA fragmentation. EAPB0503 also reduces the levels of BCR-ABL protein .
    EAPB0503
  • 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
  • HY-12292G
    IM-12 (GMP)
    		Antagonist
    IM-12 GMP is IM-12 (HY-12292) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. IM-12 is an orally active anti-inflammatory agent that targets and inhibits the NF-κB and STAT3 signaling pathways. IM-12 activates the Wnt signaling pathway and promotes the nuclear translocation of β-catenin by inhibiting GSK3β, while also blocking the tyrosine kinase activity of p210BCR/ABL. IM-12 reduces the levels of IL-6, IL-17, NO, prostaglandin E2, iNOS and COX-2, and induces ER stress, Ca2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABLT315I mutant cells. IM-12 is also a component of the 5iLA medium used for naive pluripotent stem cell research. IM-12 has been applied in studies related to carrageenan (HY-125474)-induced hind paw edema, TNBS-induced colitis, and acute and chronic myeloid leukemia.
    IM-12 (GMP)
  • HY-155288
    DosatiLink-1
    		Inhibitor
    DosatiLink-1 is an Abelson murine leukemia (ABL) enzyme inhibitor.
    DosatiLink-1
  • HY-180925
    Leu-PEG1-Dasa
    		Degrader
    Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML).
    Leu-PEG1-Dasa
  • HY-155112
    Antiproliferative agent-30
    		Inhibitor
    Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation.
    Antiproliferative agent-30
  • HY-10181GL
    Dasatinib (GMP Like)
    		Inhibitor
    Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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 (GMP Like)
  • HY-180218
    DS-PPE-GW
    		Degrader
    DS-PPE-GW is a BCR-ABL ATTEC degrader. DS-PPE-GW connects BCR-ABL and LC3B, thereby tethering BCR-ABL to the autophagosome membrane. DS-PPE-GW shows potent BCR-ABL degradation. DS-PPE-GW has anticancer activity against chronic myeloid leukemia (Pink: LC3B ligand (HY-10542); Blue: BCR-ABL ligand (HY-107447); Black: Linker (HY-W001860)).
    DS-PPE-GW
  • HY-161323
    FLT3-ITD/D835Y-IN-1
    		Inhibitor
    FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and BCR-ABL inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML).
    FLT3-ITD/D835Y-IN-1
  • HY-180798
    BCR-ABL degrader 1
    		Degrader
    BCR-ABL degrader 1 (Compound 23) is a HyT-based BCR-ABL degrader with a DC50 of 19.9 μM. BCR-ABL degrader 1 can be used in the research of chronic myeloid leukemia.
    BCR-ABL degrader 1
  • HY-E70640
    ABL1 T315I Recombinant Human Active Protein Kinase
    The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 T315I Recombinant Human Active Protein Kinase is a recombinant ABL1 T315I protein that can be used to study ABL1 T315I-related functions.
    ABL1 T315I Recombinant Human Active Protein Kinase
  • HY-180985
    Azo-PROTAC-4C-cis
    		Degrader
    Azo-PROTAC-4C-cis is a BCR-ABL PROTAC degrader, and its degradation efficiency of BCR-ABL is much lower than that of its trans isomer Azo-PROTAC-4C-trans (HY-180983). Azo-PROTAC-4C-cis is the product of the conformational transformation of Azo-PROTAC-4C-trans under ultraviolet (UV) light irradiation. Azo-PROTAC-4C-cis can be converted into highly active Azo-PROTAC-4C-trans under visible light, thereby initiating protein degradation. Azo-PROTAC-4C-cis can be used for the study of myeloid leukemia.
    Azo-PROTAC-4C-cis
  • HY-170846
    FGFRs-IN-1
    		Inhibitor
    FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
    FGFRs-IN-1
  • HY-E70638
    ABL1 M351T Recombinant Human Active Protein Kinase
    The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 M351T Recombinant Human Active Protein Kinase is a recombinant ABL1 M351T protein that can be used to study ABL1 M351T-related functions.
    ABL1 M351T Recombinant Human Active Protein Kinase
  • HY-172096
    cSRC/BCR-ABL-IN-1
    		Inhibitor
    cSRC/BCR-ABL-IN-1 (compound 21b) is a potent Bcr-Abl and C-Src inhibitor with IC50 values of 56.2, 101 nM for Bcr-Abl, C-Src, respectively. cSRC/BCR-ABL-IN-1 shows cytotoxicity activity.
    cSRC/BCR-ABL-IN-1
  • HY-18814
    WB-BC-15
    		Inhibitor
    WB-BC-15 (WGB-BC-15) is a c-Abl kinase inhibitor. WB-BC-15 can increase radiation-induced germ-cell apoptosis, with EC50 of 10.5 μM.
    WB-BC-15
  • HY-157389
    AK-HW-90
    		Inhibitor
    AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-AblT315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML).
    AK-HW-90
  • HY-10364
    AP24163
    		Inhibitor
    AP24163 is a BCR-ABL kinase inhibitor. AP24163 inhibits wild-type (native) BCR-ABL and BCR-ABL-T315I with IC50 values of 7 nM and 511 nM, respectively. AP24163 can be used in the research of chronic myeloid leukemia (CML).
    AP24163
  • HY-179247
    BCR-ABL1-IN-2
    		Inhibitor
    BCR-ABL1-IN-2 (compound 8) is a potent BCR-ABL1 tyrosine kinase inhibitor. BCR-ABL1-IN-2 exhibits activity in Imatinib (HY-15463) resistant K562/DOX cells with LC50 of 5.29 μM. BCR-ABL1-IN-2 shows no significant toxicity in nontumor cells. BCR-ABL1-IN-2 can be used for chronic myeloid leukemia research.
    BCR-ABL1-IN-2
Cat. No. Nom du produit / Synonyms Species Source
Cat. No. Nom du produit / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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