1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl

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 Related Products (46):

Cat. No. Product Name Effect Purity
  • HY-10181
    Dasatinib Inhibitor 99.85%
    Dasatinib (BMS-354825) is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6 nM, 0.8 nM, respectively. Dasatinib also inhibits Abl, Src, Fyn, c-Kit and c-KitD816V with IC50s of 2.8 nM, 79 nM and 37 nM, respectively. Dasatinib also induces apoptosis and autophagy. Dasatinib shows potently antitumor activity and has the potential for chronic myelogenous leukemia (CML) treatment.
  • HY-13520
    Nocodazole Inhibitor 98.68%
    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, and activates CRISPR/Cas9.
  • HY-12047
    Ponatinib Inhibitor 99.13%
    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.
  • HY-15463
    Imatinib Inhibitor 99.80%
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-10159
    Nilotinib Inhibitor 99.96%
    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-123390
    DB07107 Inhibitor
    DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
  • HY-15666A
    GZD824 dimesylate Inhibitor 99.20%
    GZD824 dimesylate (HQP1351 dimesylate) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC50=0.34 nM). GZD824 dimesylate has antitumor activity.
  • HY-103032
    Multi-kinase inhibitor 1 Inhibitor
    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.
  • HY-50946
    Imatinib Mesylate Inhibitor 99.91%
    Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
  • HY-10158
    Bosutinib Inhibitor 99.96%
    Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.
  • HY-13264
    Degrasyn Inhibitor 99.70%
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
  • HY-104010
    Asciminib Inhibitor 99.78%
    Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
  • HY-50514
    AT9283 Inhibitor 99.61%
    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.
  • HY-13024
    Rebastinib Inhibitor 99.91%
    Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50 of 0.8 nM and 4 nM, also inhibits SRC, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit.
  • HY-10181A
    Dasatinib hydrochloride Inhibitor 98.86%
    Dasatinib hydrochloride (BMS-354825 hydrochloride) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor, with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride has potent antitumor activity.
  • HY-10339
    KW-2449 Inhibitor 99.85%
    KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
  • HY-50868
    Bafetinib Inhibitor 99.80%
    Bafetinib is a Lyn and Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity.
  • HY-15749
    XL228 Inhibitor 99.61%
    XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
  • HY-12070
    DPH Activator 98.83%
    DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.  
  • HY-15002
    AST 487 Inhibitor 99.20%
    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
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