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Bcr-Abl

Items 1-50 of 106

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  1. A10108
    Saracatinib (AZD0530)

    Src/Abl inhibitor

    Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.
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  2. A15186
    Nilotinib monohydrochloride monohydrate

    Bcr-Abl inhibitor

    Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
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  3. A11200
    DCC-2036 (Rebastinib)

    Bcr-Abl inhibitor

    DCC-2036 is an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity.

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  4. A10290
    Dasatinib (BMS-354825)

    Abl-Src inhibitor

    Dasatinib (BMS-354825) is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor. The main targets of dasatinib, are BCR/ABL, Src, c-Kit, ephrin receptors, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2.
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  5. A10468
    Imatinib Mesylate

    Bcr-Abl inhibitor

    Imatinib mesylate, a selective tyrosine kinase inhibitor, induced a sustained objective response in treating gastrointestinal stromal tumors with the inhibition of the KIT signal-transduction pathway.
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  6. A16320
    Dasatinib Monohydrate
    Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
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  7. A10988
    WP1130 (Degrasyn)

    DUB/Bcr/ABL Inhibitor

    WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells.
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  8. A10644
    Nilotinib (AMN-107)

    Bcr-Abl inhibitor

    Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
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  9. A10259
    Imatinib (Gleevec)

    PDGFR inhibitor

    Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.
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  10. A10661
    NVP-BHG712

    EphB4 inhibitor

    NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
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  11. A10095
    AT9283

    Aurora/JAK inhibitor

    AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
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  12. A10080
    AP24534 (Ponatinib)

    BCR-ABL inhibitor

    AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
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  13. A10715
    Danusertib (PHA-739358)

    Aurora inhibitor

    Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
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  14. A10119
    Bafetinib (INNO-406)

    Bcr-Abl inhibitor

    Bafetinib ((INNO-406) is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia.
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  15. A12421
    CHMFL-ABL/KIT-155

    ABL/c-KIT dual kinase inhibitor

    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor.
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  16. A12496
    BCR-ABL-IN-1

    BCR-ABL 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.
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  17. A13029
    Radotinib (IY-5511)

    Bcr-Abl tyrosine inhibitor?€?

    Radotinib is a novel and selective Bcl-Abl tyrosine kinase inhibitor
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  18. A13069
    XL-228

    IGF-1R, Aurora, FGFR, ABL, SRC inhibitor

    XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
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  19. A13120
    PD173955

    Bcr-Abl inhibitor

    PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth.
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  20. A13182
    CHMFL-ABL-039

    BCR-ABL inhibitor

    CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.
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  21. A13237
    GNF-5

    Bcr-Abl inhibitor

    GNF-5 is a selective allosteric inhibitor of BCR-ABL.
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  22. A11207
    PP121

    PI3K Inhibitor

    PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).
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  23. A11262
    Cenisertib

    multi-kinase inhibitor

    Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.
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  24. A11379
    DPH

    c-ABL activitor

    DPH is a c-ABL activitor.
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  25. A11439
    GNF 2

    Bcr-Abl inhibitor

    GNF 2 is a Bcr-abl inhibitor that inhibits proliferation and induces apoptosis in Bcr-abl-expressing cells.
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  26. A13530
    Flumatinib mesylate

    c-Abl/c-Kit/PDGRFβ inhibitor

    Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
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  27. A13562
    NRC-AN-019

    Bcr-Abl inhibitor

    NRC-AN-019 is an orally administered tyrosine kinase inhibitor (TKI) of the Bcr-Abl protein-tyrosine kinase. NRC-AN-019 is more effective in inhibiting angiogenic potential and proliferation of both MDAMB231 and HTB20/BT474 cells.
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  28. A15849
    GZD824 Dimesylate (Olverembatinib dimesylate)

    Bcr-Abl Inhibitor

    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.
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  29. A15887
    GNF-7

    Bcr-Abl inhibitor

    GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
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  30. A16258
    Flumatinib

    multi-kinase inhibitor

    Flumatinib is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRbeta and c-Kit respectively.
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  31. A16264
    Olverembatinib (GZD824)

    Bcr-Abl inhibitor

    GZD824 is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I.
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  32. A16265
    Lyn-IN-1

    dual Bcr-Abl/Lyn inhibitor

    Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.
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  33. A16266
    ON 146040

    dual PI3K and BCR-ABL inhibitor

    ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM.
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  34. A21043
    BCR-ABL-IN-2

    BCR-ABL inhibitor

    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
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  35. A19607
    SNIPER(ABL)-024
    SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
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  36. A19742
    CT-721

    Bcr-Abl kinase inhibitor

    CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.
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  37. A18567
    SNIPER(ABL)-062

    ABL inhibitor

    SNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein.
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  38. A19079
    CHMFL-ABL-121

    ABL2 inhibitor

    CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
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  39. A19444
    CZC-8004

    ABL inhibitor

    CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
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  40. A19488
    AZD0424

    Src/Abl kinase inhibitor

    AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
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  41. A15003
    AST 487

    RET kinase inhibitor

    AST487 is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
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  42. A30609
    PD180970

    p210Bcr-Abl Kinase Inhibitor

    PD180970 is a potent ATP-competitive inhibitor of the p210Bcr-Abl kinase, exhibiting an IC50 of 5 nM for the inhibition of its autophosphorylation. Additionally, it inhibits Src and KIT kinases with IC50 values of 0.8 nM and 50 nM, respectively. PD180970 effectively induces apoptosis in K562 leukemic cells, making it a valuable reagent for research on chronic myelogenous leukemia.
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  43. A30829
    Adaphostin

    p210bcr/abl Inhibitor

    Adaphostin, a potent inhibitor of the p210bcr/abl fusion protein (IC50 = 14 μM), exhibits significant anti-leukemic activity. It induces apoptosis in T-lymphoblastic leukemia cell lines, with IC50 values ranging from 17 to 216 nM. This compound demonstrates selective efficacy against both chronic and acute myeloid leukemia cells and increases reactive oxygen species (ROS) levels in chronic lymphocytic leukemia (CLL) B cells, making it valuable for research in leukemia therapeutics and cellular pathways related to oxidative stress.
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  44. A30844
    HG-7-85-01

    Bcr-Abl Inhibitor

    HG-7-85-01 is a type II ATP competitive inhibitor that targets Bcr-Abl, including its T315I mutant, as well as PDGFRα, Kit, and Src kinases. It demonstrates potent inhibition with IC50 values of 3 nM for T315I Bcr-Abl, 20 nM for KDR, and 30 nM for RET, while showing minimal activity against other kinases (IC50 > 2 μM). HG-7-85-01 effectively inhibits cell proliferation through the induction of apoptosis and the suppression of cell-cycle progression, making it a valuable tool for research in cancer biology.
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  45. A33377
    Debio 0617B

    Multi-kinase Inhibitor

    Debio 0617B is a multi-kinase inhibitor that targets key kinases involved in the regulation of STAT3/STAT5 signaling, including JAK, SRC, ABL, and class III/V receptor tyrosine kinases. This compound effectively reduces the maintenance and self-renewal of primary human acute myeloid leukemia (AML) CD34+ stem/progenitor cells. Additionally, Debio 0617B has demonstrated efficacy in preclinical models of STAT3-driven solid tumors, making it a valuable tool for cancer research and therapeutic development.
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  46. A33588
    AFG210

    Abl Kinase Inhibitor

    AFG210 is a potent Abl kinase inhibitor with an IC50 of 330 nM, demonstrating significant inhibitory effects on additional kinases including B-Raf, C-Raf, FGFR-1, RET, and VEGF receptors. Its unique multi-target profile positions AFG210 as a valuable tool for investigating chronic myeloid leukemia and other disorders associated with aberrant Abl kinase activation. This compound facilitates research exploring targeted therapies and signaling pathways linked to these diseases.
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  47. A33591
    Leu-PEG1-Dasa

    BCR-ABL PROTAC Degrader

    Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy.
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  48. A33592
    PD166326

    Bcr/Abl Kinase Inhibitor

    PD166326 is a potent Bcr/Abl kinase inhibitor with an IC50 of 8 nM for Abl tyrosine kinase and 6 nM for Src tyrosine kinase. This compound effectively blocks Bcr/Abl kinase activity, leading to the inhibition of Bcr/Abl-dependent cell proliferation and cell cycle progression. In preclinical studies, PD166326 has demonstrated the ability to reduce peripheral blood granulocytosis, alleviate splenomegaly, and prolong survival in mouse models of chronic myeloid leukemia. It serves as a valuable tool for research focused on chronic myeloid leukemia and related signaling pathways.
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  49. A33594
    Asciminib hydrochloride

    BCR-ABL1 Inhibitor

    Asciminib hydrochloride is a potent and selective allosteric inhibitor targeting BCR-ABL1. This compound demonstrates significant biological activity by inhibiting Ba/F3 cells with an IC50 of 0.25 nM. Asciminib is primarily utilized in research applications focusing on chronic myeloid leukemia and other BCR-ABL1 driven malignancies, providing valuable insight into the mechanisms of resistance and therapeutic strategies.
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  50. A33596
    Nilotinib-d6

    Bcr-Abl Inhibitor

    Nilotinib-d6 is a deuterated form of Nilotinib, a selective inhibitor of the Bcr-Abl tyrosine kinase. This compound exhibits antineoplastic activity, making it valuable in the study of chronic myeloid leukemia and other malignancies characterized by Bcr-Abl expression. Nilotinib-d6 is particularly useful in pharmacokinetic studies and metabolic profiling due to its unique isotopic labeling.
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