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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Risvodetinib
0 ImagesSynonyms: IkT-148009Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD.
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N-Desmethyl imatinib
0 ImagesSynonyms: Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.
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GMB-475
0 ImagesGMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia.
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Olverembatinib dimesylate
0 ImagesSynonyms: GZD824 dimesylate; HQP1351 dimesylateOlverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity. Olverembatinib (dimesylate) 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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GNF-5
0 ImagesGNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.
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Dasatinib-d8
0 ImagesSynonyms: BMS-354825-d8
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GNF-7
0 ImagesGNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
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Bosutinib hydrate
0 ImagesSynonyms: SKI-606 hydrateBosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
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PD180970
0 ImagesPD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.
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L18I
0 ImagesL18I is a Bruton's tyrosine kinase (BTK) PROTAC degrader that targets wild-type and BTKC481, and recruits the cereblon E3 ligase to mediate proteasomal degradation. L18I regulates the BCR, TLR, FcγR and NLRP3 inflammasome signaling pathways, inhibits the phosphorylation of PLCγ-2, ERK1/2 and p38, and reduces the levels of B cell activation markers CD25, CD69 and CD86. L18I downregulates the NF-κB, TNF and TLR signaling pathways, reduces the production of pro-inflammatory cytokines, and decreases immune cell infiltration and immune complex deposition. L18I inhibits the proliferation of BTK-expressing lymphoma cells, induces tumor regression in xenograft models, and exhibits synergistic activity when combined with inhibitors of SYK, PI3K or Lyn. L18I can be used in research related to lupus, diffuse alveolar hemorrhage and B-cell lymphoma.
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PROTAC BCR-ABL Degrader-1
0 ImagesPROTAC BCR-ABL Degrader-1 is a PROTAC degrader targeting BCR-ABL, and also selectively inhibits cancer cell proliferation. PROTAC BCR-ABL Degrader-1 induces degradation via the ubiquitin-proteasome system to reduce protein levels. PROTAC BCR-ABL Degrader-1 can be used for research on chronic myeloid leukemia.
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Vamotinib
0 ImagesSynonyms: PF-114Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABLT315I), 9.5 nM (ABLE255K), 2.0 nM (ABLF317I), 7.4 nM (ABLG250E), 1.0 nM (ABLH396P), 2.8 nM (ABLM351T), 12 nM (ABLQ252H), and 4.1 nM (ABLY253F), respectively. Vamotinib 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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Imatinib-d4
0 ImagesSynonyms: STI571 d4; CGP-57148B d4
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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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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.
