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. 상품명 효과 Purity Chemical Structure
  • HY-146528
    c-ABL-IN-3
    		Inhibitor
    c-ABL-IN-3 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-3 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 50).
    c-ABL-IN-3
  • HY-119177
    PD173956
    		Inhibitor
    PD173956 is a pyridopyrimidine Bcr-Abl kinase inhibitor with high selectivity for the P-loop mutant form of Bcr-Abl.
    PD173956
  • HY-125142
    AP-24567
    		Inhibitor
    AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).
    AP-24567
  • HY-177272
    HPK1-IN-61
    		Inhibitor
    HPK1-IN-61 (Compound 1) is an inhibitor of hematopoietic progenitor kinase 1 (HPK1) (Ki = 0.4 nM) and an inhibitor of Abl (IC50 < 0.51 nM). HPK1-IN-61 also shows inhibitory activity against LCK with an IC50 of 24 nM.
    HPK1-IN-61
  • HY-185658
    3'-BPANeuGc
    		Inhibitor
    3'-BPANeuGc is a high-affinity selective Siglec-G ligand. Lipid nanoparticles surface-modified with antigens and 3'-BPANeuGc inhibit BCR signal transduction. 3'-BPANeuGc is applicable to antigen-specific tolerance research.
    3'-BPANeuGc
  • HY-180968
    GMB-805
    		Degrader
    GMB-805 is a BCR-Abl PROTAC degrader with a DC50 of 30 nM in K562 cells. GMB-805 exerts antiproliferative activity in K562 cells. GMB-805 exhibits potent anti-tumor activity with favorable safety profile in vivo. GMB-805 can be used for chronic myeloid leukemia research.
    GMB-805
  • HY-182792
    Embibatinib
    		Inhibitor
    Embibatinib (TERN-701) (Compound 1) is a highly selective, orally effective BCR-ABL allosteric inhibitor. Embibatinib is applicable for cancer research, particularly leukemia.
    Embibatinib
  • HY-118964
    Tyrphostin AG 568
    		Inhibitor
    Tyrphostin AG 568 is a tyrphostin tyrosine kinase inhibitor that induces erythroid differentiation. Tyrphostin AG 568 can be utilized in research related to autologous bone marrow transplantation.
    Tyrphostin AG 568
  • HY-18819
    BCR-ABL-IN-2
    		Inhibitor
    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
    BCR-ABL-IN-2
  • HY-180967
    PROTAC BCR-ABL Degrader-2
    		Degrader
    PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research.
    PROTAC BCR-ABL Degrader-2
  • HY-150566
    BCR-ABL-IN-5
    		Inhibitor
    BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-AblWT and Bcr-AblT3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells.
    BCR-ABL-IN-5
  • HY-186016
    Arg-PEG1-Dasa
    		Degrader
    Arg-PEG1-Dasa is a mini-PROTAC targeting BCR-ABL. Arg-PEG1-Dasa induces BCR-ABL degradation (EC50 = 0.85 nM) and shows antiproliferative activity in K562 cells (IC50 = 0.36 nM). Arg-PEG1-Dasa can be used for chronic myeloid leukemia research.
    Arg-PEG1-Dasa
  • HY-111863
    SNIPER(ABL)-047
    		Inhibitor
    SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM.
    SNIPER(ABL)-047
  • HY-171146
    HSN748
    		Inhibitor
    HSN748 is a Ponatinib (HY-12047) analogue and a multikinase inhibitor. HSN748 has inhibitory activity on FLT3, ABL1, RET, PDGFRα/β, MNK1, MNK2 and other kinases. HSN748 can inhibit the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines and can be used in the study of leukemia.
    HSN748
  • HY-169231
    BCR-ABL-IN-10
    		Inhibitor
    BCR-ABL-IN-10 (compound B4) is a covalent and aryl vinyl sulfate (AVS)-containing BCR-ABL inhibitor with an IC50 of 43.1 nM for ABL kinase. BCR-ABL-IN-10 forms a covalent and stable adduct with ABL kinase, leading to sustained inhibition of endogenous BCR-ABL activities. BCR-ABL-IN-10 can be used for the study of chronic myeloid leukemia (CML).
    BCR-ABL-IN-10
  • HY-183103
    PDD-87
    		Inhibitor
    PDD-87 is an orally active, blood-brain barrier permeable kinase inhibitor, with IC50 values ranging from 0.07 nM to 0.72 nM against ABL, SRC family, BTK kinases and their key mutants. PDD-87 induces antiproliferative effects in leukemia and lymphoma cells, and inhibits tumor growth in mouse xenograft models. PDD-87 can be used for the research of leukemia and lymphoma.
    PDD-87
  • HY-108417
    Debio 0617B
    		Inhibitor
    Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34+ stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors.
    Debio 0617B
  • HY-14979A
    ML786 dihydrochloride
    		Inhibitor
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
    ML786 dihydrochloride
  • HY-125090
    PHA-680626
    		Inhibitor
    PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells.
    PHA-680626
  • HY-15268
    PP487
    		Inhibitor
    PP487 is a selective dual inhibitor of Tyrosine kinase/PI3-K, with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used in cancer research.
    PP487
Cat. No. 상품명 / Synonyms Species Source
Cat. No. 상품명 / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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