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-13905
    Flumatinib mesylate
    		Inhibitor 99.80%
    Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model.
    Flumatinib mesylate
  • HY-153996
    CT1113
    		Inhibitor 99.61%
    CT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia.
    CT1113
  • HY-13520R
    Nocodazole (Standard)
    		Inhibitor
    Nocodazole (Standard) is the analytical standard of Nocodazole. This product is intended for research and analytical applications. Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl.
    Nocodazole (Standard)
  • HY-10159C
    Nilotinib hydrochloride dihydrate
    		Inhibitor 99.89%
    Nilotinib (AMN107) hydrochloride dihydrate is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia.
    Nilotinib hydrochloride dihydrate
  • HY-101489A
    GZD856 formic
    		Inhibitor
    GZD856 formic is a potent and orally active PDGFRα/β 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 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GZD856 formic
  • HY-13904S
    Flumatinib-d3
    		Inhibitor 99.9%
    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-123450
    S116836
    		Inhibitor 99.78%
    S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies. S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    S116836
  • HY-117718
    AG957
    		Inhibitor 99.30%
    AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity.
    AG957
  • HY-157327
    AKE-72
    		Inhibitor 98.29%
    AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL. AKE-72 inhibits BCR-ABLWT, BCR-ABLT315, BCR-ABLE255K, BCR-ABLF3171, BCR-ABLH396P and BCR-ABLQ252H with IC50s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line.
    AKE-72
  • HY-145887
    BCR-ABL1-IN-1
    		99.82%
    BCR-ABL1-IN-1 (Example 74) is the inhibitor for ABL1 (64-515) with IC50 of 8.7 nM. BCR-ABL1-IN-1 can be used in research on diseases related to the central nervous system (CNS).
    BCR-ABL1-IN-1
  • HY-10181R
    Dasatinib (Standard)
    		Inhibitor
    Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-164393
    ON044580
    		Inhibitor 99.11%
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.
    ON044580
  • HY-15463R
    Imatinib (Standard)
    		Inhibitor
    Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib (Standard)
  • HY-P5426
    Abl protein tyrosine kinase substrate
    		Substrate 99.70%
    Abl protein tyrosine kinase substrate is a biological active peptide. (Abltide is a peptide substrate for Abl Kinase (Abl protein tyrosine kinase), a partner in the gag-Abl fusion protein of the Abelson murine leukemia virus. Used in Western blot and kinase assay.)
    Abl protein tyrosine kinase substrate
  • HY-176461
    Pro-Dasatinib
    		Inhibitor
    Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib (HY-10181), is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC50 of 0.21 nM.
    Pro-Dasatinib
  • HY-12083
    PPY-A
    		Inhibitor 98.02%
    PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML).
    PPY-A
  • HY-161057
    HG-7-86-01
    		Inhibitor 98.41%
    HG-7-86-01 (Compound 26) is type II tyrosine kinase inhibitor. HG-7-86-01 has anti-proliferative activity.
    HG-7-86-01
  • HY-117291A
    XMD-17-51 TFA
    		99.46%
    XMD-17-51 TFA is a pyrimido-diazepinone compound that is able to modulate protein kinases.
    XMD-17-51 TFA
  • HY-131178
    HG-7-85-01-NH2
    		98.05%
    HG-7-85-01-NH2 is the HG-7-85-01 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
    HG-7-85-01-NH2
  • HY-10159R
    Nilotinib (Standard)
    		Inhibitor
    Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Bcr-Abl Isoform Comparison

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