| S1490 |
Ponatinib (AP24534)
|
Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
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Nat Commun, 2025, 16(1):471
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Theranostics, 2025, 15(8):3589-3609
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J Exp Clin Cancer Res, 2025, 44(1):290
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| S5254 |
Dasatinib hydrochloride
|
Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
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Clin Transl Med, 2024, 14(5):e1660
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Cell Death Dis, 2024, 15(8):603
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iScience, 2024, 27(10):110862
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| S1021 |
Dasatinib (BMS-354825)
|
Dasatinib 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 in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
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Cancer Cell, 2025, S1535-6108(25)00070-4
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Mil Med Res, 2025, 12(1):83
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Nat Commun, 2025, 16(1):4069
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| S2475 |
Imatinib (STI571)
|
Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
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Cancer Cell, 2025, 43(4):776-796.e14
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Theranostics, 2025, 15(8):3589-3609
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Genome Med, 2025, 17(1):14
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| S2775 |
Nocodazole
|
Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
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Adv Mater, 2025, e17493.
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Nat Commun, 2025, 16(1):7898
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EMBO J, 2025, 44(22):6556-6597
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| S1026 |
Imatinib (STI571) Mesylate
|
Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
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Sci Immunol, 2025, 10(109):eads5818
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Blood Adv, 2025, bloodadvances.2024015364
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Eur J Med Chem, 2025, 284:117211
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| S1033 |
Nilotinib
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Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. This compound induces autophagy through AMPK activition.
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Blood Adv, 2025, bloodadvances.2024015364
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Cell Death Discov, 2025, 11(1):62
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Immunology, 2025, NONE
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| S2243 |
Degrasyn (WP1130)
|
Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). This compound induces apoptosis and blocks autophagy.
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Nat Commun, 2025, 16(1):628
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Nat Commun, 2025, 16(1):1313
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Cell Death Dis, 2025, 16(1):564
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| S5205 |
Nilotinib hydrochloride
|
Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
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Nat Commun, 2024, 15(1):2089
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J Pharm Sci, 2022, 111(8):2180-2190
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EMBO Mol Med, 2021, e11814
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| S1369 |
Bafetinib
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Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.
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Elife, 2024, 12RP92324
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Br J Haematol, 2023, 10.1111/bjh.18996
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Int J Mol Sci, 2023, 10.3390/ijms241813863
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