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Formula | C26H29Cl2N5O3 |
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Molecular Weight | 530.45 | CAS No. | 380843-75-4 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (188.51 mM) | |
Ethanol | 9 mg/mL (16.96 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. | |||||||||||
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In vitro | Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. [1] Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. [2] Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin. [3] |
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In vivo | Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. [1] Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. [2] As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts. [4] |
Kinase Assay: |
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Data from [J Virol, 2011, 85, 2296–2303]
Data from [J Biol Chem, 2010, 285, 7977–7985]
, , Mol Cancer Ther, 2017, 16(6):1145-1154
, , Dr. Pablo E.Visconti from University of Massachusetts
The molecular basis of Abelson kinase regulation by its αI-helix [ Elife, 2024, 12RP92324] | PubMed: 38588001 |
hFcγRIIa: a double-edged sword in osteoclastogenesis and bone balance in transgenic mice [ Front Immunol, 2024, 15:1425670] | PubMed: 39281679 |
Merkel cell polyomavirus protein ALTO modulates TBK1 activity to support persistent infection [ PLoS Pathog, 2024, 20(7):e1012170] | PubMed: 39074144 |
Asciminib Maintains Antibody-Dependent Cellular Cytotoxicity against Leukemic Blasts [ Cancers (Basel), 2024, 16(7)1288] | PubMed: 38610966 |
Neratinib plus dasatinib is highly synergistic in HER2-positive breast cancer in vitro and in vivo [ Transl Oncol, 2024, 49:102073] | PubMed: 39191139 |
HIF-1α-dependent upregulation of angiogenic factors by mechanical stimulation in retinal pigment epithelial cells [ Dis Model Mech, 2024, 17(4)dmm050640] | PubMed: 38691000 |
The E156K mutation in the CRYAA gene affects the epithelial-mesenchymal transition and migration of human lens epithelial cells [ Heliyon, 2024, 10(1):e23690] | PubMed: 38187316 |
A semiconductor 96-microplate platform for electrical-imaging based high-throughput phenotypic screening [ Nat Commun, 2023, 14(1):7576] | PubMed: 37990016 |
Multiplexed kinase interactome profiling quantifies cellular network activity and plasticity [ Mol Cell, 2023, 83(5):803-818.e8] | PubMed: 36736316 |
Combination Therapies with CDK4/6 Inhibitors to Treat KRAS-Mutant Pancreatic Cancer [ Cancer Res, 2023, 83(1):141-157] | PubMed: 36346366 |
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