Bcr-Abl
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
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Bcr-Abl Inhibitors
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Bcr-Abl Antagonist
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Bcr-Abl Activator
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Bcr-Abl Modulators
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Bcr-Abl Degraders
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Bcr-Abl Substrate
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ABL1 Proteins
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Bcr-Abl Related Products (248)
Related Products (248)
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Recombinant Proteins (6)
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Antibodies (6)
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Bcr-Abl Isoform Comparison
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Adaphostin
0 ImagesSynonyms: NSC 680410Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells.
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Imatinib-d8
0 ImagesSynonyms: STI571-d8; CGP-57148B-d8
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Flumatinib mesylate
0 ImagesSynonyms: HHGV678 mesylateFlumatinib (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.
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CT1113
0 ImagesCT1113 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.
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Nocodazole (Standard)
0 ImagesSynonyms: Oncodazole (Standard); R17934 (Standard)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.
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GZD856 formic
0 ImagesCat. No.: HY-101489ACAS No.: 2804039-78-7GZD856 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.
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S116836
0 ImagesS116836, 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.
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AG957
0 ImagesSynonyms: Tyrphostin AG957; NSC 654705AG957 (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.
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ON044580
0 ImagesON044580 is a non–ATP-competitive JAK2 and BCR-ABL kinases inhibitor. ON044580 inhibits wild-type (WT) and V617F mutant JAK2 with IC50 values of 1.23 μM, 1.09 μM, respectively. ON044580 also inhibits both WT and T315I mutant BCR-ABL kinases., ON044580 blocks the IL-3–mediated phosphorylation of JAK2 and STAT5, induces apoptosis in Imatinib (HY-15463)-resistant chronic myeloid leukemia (CML). ON044580 can be used for the study of CML, myelodysplasia (MDS) and other myeloproliferative neoplasms.
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Dasatinib (Standard)
0 ImagesSynonyms: BMS-354825 (Standard)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.
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Imatinib (Standard)
0 ImagesSynonyms: STI571 (Standard); CGP-57148B (Standard)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.
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Abl protein tyrosine kinase substrate
0 ImagesAbl 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.)
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PPY-A
0 ImagesPPY-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).
