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-155288
    DosatiLink-1
    		Inhibitor
    DosatiLink-1 is an Abelson murine leukemia (ABL) enzyme inhibitor.
    DosatiLink-1
  • HY-13904S
    Flumatinib-d3
    		Inhibitor
    Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
    Flumatinib-d<sub>3</sub>
  • 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-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-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-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-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-P1785
    Abl Cytosolic Substrate
    		99.60%
    Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ). Abl Protein Tyrosine Kinase (AbI) is a truncated form of the v-AbI Protein Tyrosine Kinase, a partner in the Gag-Abl fusion protein of the Abelson murine leukemia virus.
    Abl Cytosolic Substrate
  • 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-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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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