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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Adaphostin (Standard)
0 ImagesSynonyms: NSC 680410 (Standard)Adaphostin (Standard) is the analytical standard of Adaphostin. This product is intended for research and analytical applications. Adaphostin (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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KW-2449 (Standard)
0 ImagesCat. No.: HY-10339RCAS No.: 1000669-72-6
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HS-438
0 ImagesCat. No.: HY-123486CAS No.: 1430720-10-7HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML).
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Multi-kinase inhibitor 1 (Standard)
0 ImagesCat. No.: HY-103032RCAS No.: 778274-97-8Multi-kinase inhibitor 1 (Standard) is the analytical standard of Multi-kinase inhibitor 1 (HY-103032). This product is intended for research and analytical applications. Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
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BCR-ABL-IN-11
0 ImagesBCR-ABL-IN-11 (Compound 2) is a BCR-ABL inhibitor. BCR-ABL-IN-11 shows anticancer activity against chronic myelogenous leukemia (CML) (IC50 of 129.61 μM for K562 cells).
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AFG210
0 ImagesCat. No.: HY-18817CAS No.: 228400-22-4AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.
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Enzyme modulator-1
0 ImagesCat. No.: HY-186223CAS No.: 897375-76-7Enzyme modulator-1 (example 205) is a potent enzyme modulator that modulates p38, bcr-ab1, and VEGFR. Enzyme modulator-1 can be used for the research of cancer, rheumatoid arthritis, retinopathies including diabetic retinal neuropathy and macular degeneration.
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Ponatinib (Standard)
0 ImagesSynonyms: AP24534 (Standard)Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
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Ponatinib hydrochloride (Standard)
0 ImagesSynonyms: AP24534 hydrochloride (Standard)Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
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AN-019
0 ImagesCat. No.: HY-15493CAS No.: 879507-25-2Synonyms: NRC-AN-019AN-019 is a Bcr-Abl kinase inhibitor. AN-019 has antitumor activity.
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BCR-ABL kinase-IN-3 (dihydrocholide)
0 ImagesCat. No.: HY-160174ABCR-ABL kinase-IN-3 (dihydrocholide) (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research.
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PD173955 (Standard)
0 ImagesPD173955 (Standard) is the analytical standard of PD173955 (HY-10395). This product is intended for research and analytical applications. PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity.
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AT9283 (Standard)
0 ImagesAT9283 (Standard) is the analytical standard of AT9283. This product is intended for research and analytical applications. AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
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Nilotinib monohydrochloride monohydrate (Standard)
0 ImagesSynonyms: AMN107 monohydrochloride monohydrate (Standard)Nilotinib (monohydrochloride monohydrate) (Standard) is the analytical standard of Nilotinib (monohydrochloride monohydrate). This product is intended for research and analytical applications. Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
