bcr-abl

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

AN-019 (NRC-019) is a Bcr-Abl kinase inhibitor with antitumor activity for the study of chronic myelogenous leukemia (CML) and breast cancer.

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor with oral activity. Nilotinib has antitumor activity and may be used for the treatment of Imatinib-resistant chronic myelogenous leukemia (CML).

Bafetinib (INNO-406) (INNO-406) is an effective and specific dual Bcr-Abl Lyn inhibitor (IC50: 5.8 19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

Nocodazole (Oncodazole) is a reversible inhibitor of microtubule polymerization and an inhibitor of Bcr-Abl. Nocodazole has antitumor activity, blocks the cell cycle and induces apoptosis.

BCR-ABL-IN-11 (Compound 2) is an inhibitor of BCR-ABL, exhibiting anticancer activity against chronic myelogenous leukemia (CML) with an IC50 value of 129.61 μM in K562 cells.

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor characterized by a trimethoxy group [1].

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

cSRC BCR-ABL-IN-1 (compound 21b) is a potent inhibitor of Bcr-Abl and C-Src, with IC50 values of 56.2 nM and 101 nM, respectively. It exhibits cytotoxicity.

Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.

BCR-ABL-IN-10 (compound B4) is a covalent BCR-ABL inhibitor featuring an arylvinylsulfonate (AVS) moiety, demonstrating an IC50 of 43.1 nM against ABL kinase. It forms a covalent and stable adduct with ABL kinase, enabling the sustained inhibition of intrinsic BCR-ABL activity. This compound is utilized in the study of chronic myeloid leukemia (CML).

BCR-ABL-IN-9 (Compound B1) is an inhibitor of BCR-ABL that achieves sustained suppression through the formation of stable covalent bonds with the ABL kinase. It effectively inhibits the activity of ABL kinase (IC50 = 1.2 nM) and possesses anticancer activity.

BCR-ABL-IN-7 is a WT and T315I mutant ABL kinase inhibitor.BCR-ABL-IN-7 potently inhibits WT and T315I mutant ABL kinase activity.BCR-ABL-IN-7 can be used in chronic myelogenous leukemia (CML) research.

BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.

BCR-ABL-IN-4 is a BCR-ABL inhibitor exhibiting anticancer activity with an inhibitory effect on cancer cell growth, specifically on K562 cells (IC50: 0.67 nM) and BCR-ABL T315I-transfected Ba F3 cells (IC50: 16 nM).

PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, induces Bcr-Abl degradation via the ubiquitin-proteasome pathway and exhibits antiproliferative effects on K562 cells, indicating its potential in cancer research [1].

BCR-ABL-IN-6 (9h) is an imatinib derivative and a selective inhibitor of Bcr-Abl kinase, showing activity on Bcr-AblWT (IC50: 4.6 nM) and Bcr-AblT3151 (IC50: 277 nM). BCR-ABL-IN-6 (9h) is utilized in studying chronic myeloid leukemia treatment.

BCR-ABL kinase-IN-3 (example 1), a potent BCR-ABL inhibitor, is significant in the study of acute myeloid leukemia (AML) [1].

BCR-ABL-IN-5 is a Bcr-Abl (Breakpoint cluster region-Abelson) kinase inhibitor that acts on Bcr-AblWT (IC50: 0.014 μM) and Bcr-AblT3151 (IC50: 0.45 μM) and exhibits some anti-proliferative effects on leukemic cells. effect.