Bcr-Abl
BCR-ABL1 is a Philadelphia chromosome-derived fusion oncogene that encodes a constitutively active tyrosine kinase and drives chronic myeloid leukemia (CML) pathophysiology[1]. Mechanistically, BCR-ABL1 coordinates malignant signaling with pathways linked to proliferation, apoptosis resistance, hematopoietic stem cell alteration, and leukemia stem cell persistence[2][3]. In disease models and clinical monitoring, CML is defined by BCR-ABL1 transcripts, most commonly e13a2 and e14a2, which encode p210 BCR-ABL1[4]. Compared with these common isoforms, rare transcripts such as e1a2, e19a2, e6a2, e8a2, e13a3, and e14a3 show structural divergence that can alter leukemogenic activity, diagnostic detection, and tyrosine kinase inhibitor response[5][6]. Transcript subtype also has practical research value, because e14a2 showed faster or deeper molecular responses than e13a2 in imatinib- or nilotinib-treated cohorts, while survival did not differ between transcripts[4]. For experimental applications, imatinib targets ABL kinase activity, whereas nilotinib and dasatinib show stronger BCR-ABL inhibition and retain activity against multiple imatinib-resistant mutants[1].
References:
- [1]. Kantarjian HM, et al. Important therapeutic targets in chronic myelogenous leukemia. Clin Cancer Res. 2007 Feb 15;13(4):1089-97. [Content Brief]
- [2]. Mencalha AL, et al. Role of calcium-dependent protein kinases in chronic myeloid leukemia: combined effects of PKC and BCR-ABL signaling on cellular alterations during leukemia development. Onco Targets Ther. 2014 Jul 8;7:1247-54. [Content Brief]
- [3]. Moradi F, et al. Signaling pathways involved in chronic myeloid leukemia pathogenesis: The importance of targeting Musashi2-Numb signaling to eradicate leukemia stem cells. Iran J Basic Med Sci. 2019 Jun;22(6):581-589. [Content Brief]
- [4]. Su YJ, et al. Comparison of molecular responses and outcomes between BCR::ABL1 e14a2 and e13a2 transcripts in chronic myeloid leukemia. Cancer Sci. 2022 Oct;113(10):3518-3527. [Content Brief]
- [5]. Zhou X, et al. The silent players: Atypical BCR‑ABL isoforms as biomarkers and therapeutic hurdles in CML pathogenesis (Review). Oncol Rep. 2025 Dec;54(6):162. [Content Brief]
- [6]. Massimino M, et al. Impact of the Breakpoint Region on the Leukemogenic Potential and the TKI Responsiveness of Atypical BCR-ABL1 Transcripts. Front Pharmacol. 2021 Jun 30;12:669469. [Content Brief]
All Product Categories
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Bcr-Abl Related Products (197)
Related Products (197)
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HPK1-IN-61
0 ImagesCat. No.: HY-177272CAS No.: 875638-86-1
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3'-BPANeuGc
0 ImagesCat. No.: HY-185658CAS No.: 1596134-81-43'-BPANeuGc is a high-affinity selective Siglec-G ligand. Lipid nanoparticles surface-modified with antigens and 3'-BPANeuGc inhibit BCR signal transduction. 3'-BPANeuGc is applicable to antigen-specific tolerance research.
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Tyrphostin AG 568
0 ImagesCat. No.: HY-118964CAS No.: 151013-48-8Tyrphostin AG 568 is a tyrphostin tyrosine kinase inhibitor that induces erythroid differentiation. Tyrphostin AG 568 can be utilized in research related to autologous bone marrow transplantation.
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PROTAC BCR-ABL Degrader-2
0 ImagesCat. No.: HY-180967CAS No.: 2703834-25-5PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research.
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BCR-ABL-IN-5
0 ImagesCat. No.: HY-150566CAS No.: 1795736-60-5
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BCR-ABL-IN-10
0 ImagesCat. No.: HY-169231BCR-ABL-IN-10 (compound B4) is a covalent and aryl vinyl sulfate (AVS)-containing BCR-ABL inhibitor with an IC50 of 43.1 nM for ABL kinase. BCR-ABL-IN-10 forms a covalent and stable adduct with ABL kinase, leading to sustained inhibition of endogenous BCR-ABL activities. BCR-ABL-IN-10 can be used for the study of chronic myeloid leukemia (CML).
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PDD-87
0 ImagesCat. No.: HY-183103CAS No.: 2222129-13-5PDD-87 is an orally active, blood-brain barrier permeable kinase inhibitor, with IC50 values ranging from 0.07 nM to 0.72 nM against ABL, SRC family, BTK kinases and their key mutants. PDD-87 induces antiproliferative effects in leukemia and lymphoma cells, and inhibits tumor growth in mouse xenograft models. PDD-87 can be used for the research of leukemia and lymphoma.
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Debio 0617B
0 ImagesCat. No.: HY-108417CAS No.: 1332329-27-7Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34+ stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors.
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PHA-680626
0 ImagesCat. No.: HY-125090CAS No.: 398493-74-8PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells.
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ABL1 F317I Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70635The 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.
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DosatiLink-2
0 ImagesCat. No.: HY-155289CAS No.: 2941512-38-3DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor.
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SIAIS100
0 ImagesCat. No.: HY-152036CAS No.: 3033463-06-5SIAIS100 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).
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ABL1 Y253F Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70641The 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.
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BCR-ABL-IN-13
0 ImagesBCR-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.
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EGFR-IN-216
0 ImagesCat. No.: HY-187334CAS No.: 1923767-20-7EGFR-IN-216 is an epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor. EGFR-IN-216 inhibits EGFR tyrosine kinase phosphorylation, blocks downstream signaling pathway activation, suppresses cancer cell proliferation and promotes tumor cell apoptosis (apoptosis). EGFR-IN-216 can be used for the research of non-small cell lung cancer.
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CpCDPK1/TgCDPK1-IN-1
0 ImagesCat. No.: HY-128397CAS No.: 1092788-23-2
