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-E70635
    ABL1 F317I 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 F317I Recombinant Human Active Protein Kinase is a recombinant ABL1 F317I protein that can be used to study ABL1 F317I-related functions.
    ABL1 F317I Recombinant Human Active Protein Kinase
  • HY-101268
    CHMFL-ABL-053
    		Inhibitor
    CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC50 values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively.
    CHMFL-ABL-053
  • HY-180963
    Lys-PEG1-Dasa
    		Degrader
    Lys-PEG1-Dasa is a BCR-ABL PROTAC degrader with an DC50 of 0.98 nM in K562 cells. Lys-PEG1-Dasa exerts growth inhibitory with IC50 of 0.4569 nM in K562 cells. Lys-PEG1-Dasa can be used for chronic myeloid leukemia research.
    Lys-PEG1-Dasa
  • HY-180981
    P19As
    		Degrader
    P19As is a BCR-ABL PROTAC degrader based on Asciminib (HY-104010), with a DC50 value of approximately 200 nM for the wild-type BCR-ABL protein. P19As can degrade the T315I mutant and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19As can be used for the study of chronic myeloid leukemia and acute lymphoblastic leukemia.
    P19As
  • HY-155289
    DosatiLink-2
    		Inhibitor
    DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor.
    DosatiLink-2
  • HY-180977
    P19P
    		Degrader
    P19P is a BCR-ABL PROTAC degrader based on Ponatinib (HY-12047), with a DC50 value of approximately 20 nM for the wild-type BCR-ABL protein. P19P can effectively degrade various drug-resistant mutants such as T315I, E255K, H396R, and V468F, and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19P maintains strong inhibitory activity against ABL (T315I), with a IC50 of 13.1 nM. P19P does not inhibit the formation of vascular lumens in HUVEC. P19P can be used for research on chronic myeloid leukemia and acute lymphoblastic leukemia.
    P19P
  • 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-E70641
    ABL1 Y253F 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 Y253F Recombinant Human Active Protein Kinase is a recombinant ABL1 Y253F protein that can be used to study ABL1 Y253F-related functions.
    ABL1 Y253F Recombinant Human Active Protein Kinase
  • HY-112404
    BCR-ABL-IN-13
    		Inhibitor 99.86%
    BCR-ABL-IN-13 is a dual c-Src and Abl inhibitor, with a Ki value of 0.55 μM against c-Src, 0.10 μM against wild-type Abl, and 0.40 μM against the AblT315I mutant. BCR-ABL-IN-13 exerts competitive/mixed-type inhibitory effects on wild-type Abl, and non-competitive inhibitory effects on the drug-resistant AblT315I mutant. BCR-ABL-IN-13 can be used for the research of chronic myeloid leukemia.
    BCR-ABL-IN-13
  • HY-128397
    CpCDPK1/TgCDPK1-IN-1
    		Inhibitor
    CpCDPK1/TgCDPK1-IN-1 (compound 7p) is a potent CpCDPK1/TgCDPK1 dual inhibitor (IC50: 10 nM and 5.0 nM respectively). CpCDPK1/TgCDPK1-IN-1 also inhibits Abl and Src (IC50: 75 nM and 65 nM respectively). CpCDPK1/TgCDPK1-IN-1 can be used for research of toxoplasmosis.
    CpCDPK1/TgCDPK1-IN-1
  • HY-162952
    cSRC/BCR-ABL1-IN-1
    		Inhibitor
    cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor.
    cSRC/BCR-ABL1-IN-1
  • HY-177273
    Kinase modulator-1
    		Inhibitor
    Kinase modulator-1 (P142, MS: m/z445) is a kinase modulator. Kinase modulator-1 can inhibit Bcr-Abl activity, especially against drug-resistant mutant kinases (such as T315I Bcr-Abl). Kinase modulator-1 can be used for cancers like chronic myelogenous leukemia (CML) research.
    Kinase modulator-1
  • HY-175437
    MRT-7612
    		Degrader
    MRT-7612 (Compound 4) is a cereblon-based tyrosine kinases molecular glue degrader. MRT-7612 significantly induces HCK and LYN degradation, with week efficacy on LCK. MRT-7612 can be used for cancers like chronic myeloid leukemia, autoimmune and chronic inflammatory diseases research.
    MRT-7612
  • HY-10158AR
    Bosutinib hydrate (Standard)
    		Inhibitor
    Bosutinib (Standard) (SKI-606 (Standard)) hydrate is the analytical standard of Bosutinib hydrate (HY-10158A). This product is intended for research and analytical applications. Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50s of 1.2 nM and 1 nM, respectively.
    Bosutinib hydrate (Standard)
  • HY-162489
    Tyrosine kinase-IN-8
    		Inhibitor
    Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia.
    Tyrosine kinase-IN-8
  • HY-180969
    SIAIS056
    		Degrader
    SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research.
    SIAIS056
  • HY-176269
    VS1150
    		Inhibitor
    VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research.
    VS1150
  • HY-13468A
    KW-2478 hydrochloride
    		Inhibitor
    KW-2478 hydrochloride is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer.
    KW-2478 hydrochloride
  • HY-175281
    SJ11646
    		Degrader
    SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
    SJ11646
  • HY-E70636
    ABL1 G250E 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 G250E Recombinant Human Active Protein Kinase is a recombinant ABL1 G250E protein that can be used to study ABL1 G250E-related functions.
    ABL1 G250E Recombinant Human Active Protein Kinase
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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