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Bcr-Abl

Bcr-Abl

Most patients with chronic myelogenous leukemia (CML) are treated in the first instance with Bcr-Abl tyrosine-kinase inhibitors (TKI). A chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome is the root cause of more than 90% of CML cases. This abnormality results from the fusion of the break point cluster (Bcr) gene at chromosome 22 with the Abelson (Abl) tyrosine kinase gene at chromosome 9, creating a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been linked to the pathogenesis of CML. The tyrosine kinase has been selectively inhibited by substances.

Bcr-Abl related products

Structure Cat No. Product Name CAS No. Product Description
ABL1 E255K Recombinant Human Active Protein Kinase V118988 ABL1 E255K Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken its binding affinity to imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 F317I Recombinant Human Active Protein Kinase V118790 ABL1 F317I Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken its binding affinity to imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 G250E Recombinant Human Active Protein Kinase V118929 ABL1 G250E Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken the binding affinity of imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 H396P Recombinant Human Active Protein Kinase V118949 ABL1 H396P Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken the binding affinity of imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 M351T Recombinant Human Active Protein Kinase V118956 ABL1 M351T Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken its binding affinity to imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 Q252H Recombinant Human Active Protein Kinase V118872 ABL1 Q252H Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken its binding affinity to imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 T315I Recombinant Human Active Protein Kinase V118971 ABL1 T315I Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken its binding affinity to imatinib mesylate, leading to resistance to imatinib mesylate.
ABL1 Y253F Recombinant Human Active Protein Kinase V118850 ABL1 Y253F Recombinant Human Active Protein Kinase Mutations in the BCR::ABL1 kinase domain (KD) weaken its binding affinity to imatinib mesylate, leading to resistance to imatinib mesylate.
AP 24149 V69652 AP 24149 926922-29-4 AP 24149 is a potent Src-Abl dual (bifunctional) inhibitor (antagonist) with IC50s of 9.1 and 3.6 nM for Src and Abl respectively.
Arg-PEG1-Dasa V110394 Arg-PEG1-Dasa 3037776-67-0 Arg-PEG1-Dasa is a miniature PROTAC that targets BCR-ABL.
Asciminib-NH2 V109138 Asciminib-NH2 3106065-83-9 Asciminib-NH2 is a BCR-ABL ligand that can be used to synthesize PROTACs, such as P19A.
Azo-PROTAC-4C-cis V109878 Azo-PROTAC-4C-cis Azo-PROTAC-4C-cis is a BCR-ABL protein degrader that exhibits significantly reduced degradation efficiency for BCR-ABL compared to its trans isomer, Azo-PROTAC-4C-trans.
Azo-PROTAC-4C-trans V110013 Azo-PROTAC-4C-trans Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that can efficiently degrade BCR-ABL fusion proteins and ABL proteins.
BCR-ABL degrader 1 V110419 BCR-ABL degrader 1 BCR-ABL degrader 1 (compound 23) is a HyT-based BCR-ABL degrader with a DC50 value of 19.9 μM.
BCR-ABL-IN-10 V94424 BCR-ABL-IN-10 BCR-ABL-IN-10 (Compound B4) is a covalent aryl vinyl sulfate (AVS) inhibitor of BCR-ABL with IC50 of 43.1 nM for ABL kinase.
BCR-ABL-IN-11 V104734 BCR-ABL-IN-11 2362-25-6 BCR-ABL-IN-11 (Compound 2) is a BCR-ABL inhibitor.
BCR-ABL-IN-3 V69651 BCR-ABL-IN-3 2240191-12-0 BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor (antagonist) with IC50 of ≤100 nM for Ba/F3Bcr-AblT3151.
BCR-ABL-IN-7 V69653 BCR-ABL-IN-7 688050-42-2 BCR-ABL-IN-7 (compound 4) is an inhibitor (blocker/antagonist) of WT and T315I mutant ABL kinase.
BCR-ABL-IN-8 V69650 BCR-ABL-IN-8 1808288-49-4 BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group.
BCR-ABL1-IN-2 V114701 BCR-ABL1-IN-2 BCR-ABL1-IN-2 (compound 8) is a potent BCR-ABL1 tyrosine kinase inhibitor.
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