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 Control
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Bcr-Abl Substrate
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Bcr-Abl Ligand
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ABL1 Proteins
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Bcr-Abl Related Products (257)
Related Products (257)
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Recombinant Proteins (8)
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Antibodies (6)
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Bcr-Abl Isoform Comparison
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Cenisertib (Standard)
0 ImagesSynonyms: AS-703569 (Standard); R-763 (Standard)Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
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Asciminib (Standard)
0 ImagesSynonyms: ABL001 (Standard)Asciminib (Standard) is the analytical standard of Asciminib. This product is intended for research and analytical applications. Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
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GZD856
0 ImagesCat. No.: HY-101489CAS No.: 1257628-64-0
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Bosutinib-13C,d3
0 ImagesCat. No.: HY-10158S1Synonyms: SKI-606-13C,d3Bosutinib-13C,d3 (SKI-606-13C,d3) is 13C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
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BCR-ABL-IN-3
0 ImagesCat. No.: HY-136526CAS No.: 2240191-12-0
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Embibatinib
0 ImagesCat. No.: HY-182792CAS No.: 2412966-86-8Synonyms: TERN-701Embibatinib (TERN-701) is an orally active and allosteric BCR-ABL1 tyrosine kinase inhibitor targeting the myristoyl pocket. Embibatinib exhibits an IC50 of 0.38 nM against ABL1 wild-type enzyme. Embibatinib can be used for the study of chronic myeloid leukemia (CML).
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CHMFL-ABL-121
0 ImagesCat. No.: HY-119370CAS No.: 2270879-07-5
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CHMFL-ABL/KIT-155
0 ImagesCat. No.: HY-101034CAS No.: 2081093-21-0Synonyms: CHMFL-ABL-KIT-155CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
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SNIPER(ABL)-033
0 ImagesCat. No.: HY-111871CAS No.: 2222354-18-7SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM (ABL inhibitor: HY-15814; ABL inhibitor activity control: HY-131178; E3 ligase ligand: HY-128808; linker: HY-130500; E3 ligase ligand + linker: HY-128819).
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CT-721
0 ImagesCat. No.: HY-108704CAS No.: 1388710-60-8CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities. CT-721 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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AZD0424
0 ImagesCat. No.: HY-112314CAS No.: 692054-06-1AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
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SNIPER(ABL)-024
0 ImagesCat. No.: HY-111861CAS No.: 2222355-77-1SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
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AT9283 lactic acid
0 ImagesCat. No.: HY-10058CAS No.: 896466-76-5
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SGX393
0 ImagesCat. No.: HY-165532CAS No.: 1030610-86-6Synonyms: SGX70393SGX393 (SGX70393) is a Bcr-Abl kinase inhibitor. SGX393 binds to the active conformation of the kinase domains of both wild-type and T315I mutant Bcr-Abl, thereby inhibiting kinase activity. SGX393 exhibits antiproliferative effects in cells expressing wild-type or T315I mutant Bcr-Abl, and suppresses T315I-driven tumor growth. SGX393 can be used for the research of chronic myeloid leukemia.
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Rebastinib tosylate
0 ImagesCat. No.: HY-13024ACAS No.: 1033893-29-6Synonyms: DCC-2036 tosylateRebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1WT and Abl1T315I, respectively. Rebastinib tosylate potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1. Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis. Rebastinib tosylate exerts anti-tumor activity in breast cancer. Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia.
