1. Protein Tyrosine Kinase/RTK
  2. 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 (27):

Cat. No. Product Name Effect Purity
  • HY-10181
    Dasatinib Inhibitor 99.84%
    Dasatinib is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.
  • HY-13520
    Nocodazole Inhibitor 99.05%
    Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, which exhibits good potency against ABL, ABL(E255K), and ABL(T315I) with IC50 values of 0.21 μM, 0.53 μM, and 0.64 μM, respectively, and increases CRISPR/Cas9-mediated editing frequencies.
  • HY-12047
    Ponatinib Inhibitor 98.96%
    Ponatinib is a potent, orally available multi-targeted kinase inhibitor with IC50 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 is a known inhibitor of the c-Kit, Bcr-Abl, and PDGFR tyrosine kinases, inhibits the SLF-dependent activation of c-Kitwt kinase with IC50 of ~100 nM, which is similar to the concentration requires for inhibition of Bcr-Abl and PDGFR.
  • HY-10159
    Nilotinib Inhibitor 99.93%
    Nilotinib is a second generation tyrosine kinase inhibitor (TKI), is significantly more potent against BCR-ABL than Imatinib, and is active against many Imatinib-resistant BCR-ABL mutants.
  • HY-100314
    BCR-ABL-IN-1 Inhibitor
    BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
  • HY-50946
    Imatinib Mesylate Inhibitor 99.90%
    Imatinib Mesylate is a known inhibitor of the c-Kit, Bcr-Abl, and PDGFR tyrosine kinases, inhibits the SLF-dependent activation of c-Kitwt kinase with IC50 of ~100 nM, which is similar to the concentration requires for inhibition of Bcr-Abl and PDGFR.
  • HY-10158
    Bosutinib Inhibitor 99.83%
    Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
  • HY-50868
    Bafetinib Inhibitor 99.27%
    Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays.
  • HY-13264
    WP1130 Inhibitor 99.72%
    WP1130 inhibits the autoactivation of Bcr-Abl by inducing its rapid down-regulation with IC50 of 1.8 μM. WP1130 also is a deubiquitinase inhibitor.
  • HY-104010
    Asciminib Inhibitor 98.75%
    Asciminib (ABL001) is a potent and selective allosteric Bcr-Abl inhibitor; inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
  • HY-10181A
    Dasatinib hydrochloride Inhibitor 98.84%
    Dasatinib hydrochloride is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.
  • HY-13024
    DCC-2036 Inhibitor 99.84%
    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-10159A
    Nilotinib monohydrochloride monohydrate Inhibitor 99.91%
    Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly more potent against BCR-ABL than Imatinib, and is active against many Imatinib-resistant BCR-ABL mutants.
  • 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-15002
    AST 487 Inhibitor 98.64%
    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.
  • HY-15749
    XL228 Inhibitor 99.58%
    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-10395
    PD173955 Inhibitor 99.04%
    PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
  • HY-12070
    DPH Activator 98.41%
    DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.  
  • HY-15666
    GZD824 Inhibitor 98.73%
    GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
Isoform Specific Products

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