Bosutinib hydrate
Based on 24 publication(s) in Google Scholar
Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 918639-08-4
- Formula: C26H31Cl2N5O4
- Molecular Weight:548.46
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications Citing Use of MedChemExpress (MCE) Bosutinib hydrate
More- Nat Commun. 2023 Apr 24;14(1):2342. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Nanobiotechnology. 2023 Mar 21;21(1):102. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Sci Adv. 2024 Dec 13;10(50):eadq4274. [Abstract]
- Biomaterials. 2024 Mar:305:122462. [Abstract]
- Int J Biol Macromol. 2024 Dec 2:138305. [Abstract]
- EPMA J. 2025 Nov 3;16(4):831-856. [Abstract]
- Drug Des Devel Ther. 2021 Sep 15:15:3915-3925. [Abstract]
- Biomacromolecules. 2024 Dec 9;25(12):7926-7950. [Abstract]
- Biomolecules. 2022 Jun 11;12(6):819. [Abstract]
- J Pathol. 2023 Jun;260(2):203-221. [Abstract]
- Front Pharmacol. 2021 Mar 8;12:644342. [Abstract]
- ACS Omega. 2023 Jun 14;8(25):22603-22612. [Abstract]
- Target Oncol. 2020 Oct;15(5):659-671. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- ACS Med Chem Lett. 2023 Dec 5;14(12):1869-1875. [Abstract]
- Life Sci Alliance. 2022 Dec 20;6(3):e202201616. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Biochem Biophys Res Commun. 2020 Feb 19;522(4):862-868. [Abstract]
- bioRxiv. 2025 February 26.
- Biomed Pharmacother. 2024 Jul 24:178:117114. [Abstract]
- Saudi J Biol Sci. 2022 Apr;29(4):2323-2328. [Abstract]
- Technical University of Munich. 24.01.2018.
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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WB
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Flow Cytometry
Biological Activity
IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).
Bosutinib hydrate is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)
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Concentration:0.1 μmol/L
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Incubation Time:72 h
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Result:Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KU812CM L xenograft model[2]
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Dosage:75 mg/kg twice daily or 150 mg/kg once daily
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Administration:Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily)
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Result:Had the therapeutic activity and produced a dose- and schedule-dependent weight loss.
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Animal Model:Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2]
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Dosage:150 mg/kg
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Administration:Bosutinib (150 mg/kg; once daily, 5 days weekly)
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Result:Decreased the rate of tumor growth and prolonged event-free survival of mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 918639-08-4
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Appearance Solid
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Molecular Weight 548.46
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Formula C26H31Cl2N5O4
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Color White to off-white
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SMILES
CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC.O
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Synonyms
SKI-606 hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (24)
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Journal Impact Factor
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Most Recent
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Nat Commun
TMEM25 inhibits monomeric EGFR-mediated STAT3 activation in basal state to suppress triple-negative breast cancer progression. [Abstract]2023 Apr 24;14(1):2342. PMID: 37095176 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Nanobiotechnology
Bosutinib high density lipoprotein nanoformulation has potent tumour radiosensitisation effects. [Abstract]2023 Mar 21;21(1):102. PMID: 36945003 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Sci Adv
2024 Dec 13;10(50):eadq4274. PMID: 39661665
Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274. [Abstract]
Bright-field microscopy images of 3D sphere cultures of MIA PaCa-2R and mKRC.1 with vehicles, MRTX849, dasatinib, DGY-06-116, and Bosutinib (0.1 μM) as well as combinations, after 7 days of treatment.
Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274. [Abstract]
The combined use of Bosutinib (0.1 μM), DGY-06-116, or Dasatinib with MRTX849 demonstrated a similar synergistic effect in mKRC.1 cells.
Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274. [Abstract]
Representative images of H&E staining of the liver, lung, pancreas, and spleen from mice bearing mKRC.1 tumors, treated with either vehicle or the combination of MRTX849 and Bosutinib.
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Biomaterials
FAK-p38 signaling serves as a potential target for reverting matrix stiffness-modulated liver sinusoidal endothelial cell defenestration. [Abstract]2024 Mar:305:122462. PMID: 38171118 -
Int J Biol Macromol
Critical role of protein kinase CK2 in chronic myeloid leukemia cells harboring the T315I BCR::ABL1 mutation. [Abstract]2024 Dec 2:138305. PMID: 39631575 -
EPMA J
Glioma angiogenesis phosphoproteome landscape and biomarker sets identified with phenome-centered multiomics toward 3P medical approaches. [Abstract]2025 Nov 3;16(4):831-856. PMID: 41312000 -
Drug Des Devel Ther
LC-MS/MS Estimation of Rociletinib Levels in Human Liver Microsomes: Application to Metabolic Stability Estimation. [Abstract]2021 Sep 15:15:3915-3925. PMID: 34552321 -
Biomacromolecules
Comparative Study of pH-Responsive and Aggregation Stability of Bosutinib-Loaded Nanogels Comprising Gelatin Methacryloyl, Carboxymethyl Dextran, and Hyaluronic Acid for Controlled Drug Delivery in Colorectal Cancer: An Extensive In Vitro Investigation. [Abstract]2024 Dec 9;25(12):7926-7950. PMID: 39504130 -
Biomolecules
Investigating the Effect of Tyrosine Kinase Inhibitors on the Interaction between Human Serum Albumin by Atomic Force Microscopy. [Abstract]2022 Jun 11;12(6):819. PMID: 35740944 -
J Pathol
Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]2023 Jun;260(2):203-221. PMID: 36825655 -
Front Pharmacol
2021 Mar 8;12:644342. PMID: 33790797 -
ACS Omega
2023 Jun 14;8(25):22603-22612. PMID: 37387790 -
Target Oncol
In Vitro Comparison of the Effects of Imatinib and Ponatinib on Chronic Myeloid Leukemia Progenitor/Stem Cell Features. [Abstract]2020 Oct;15(5):659-671. PMID: 32780298 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
ACS Med Chem Lett
Atypical N-Alkyl to N-Noralkoxy Switch in a Dual cSRC/BCR-ABL1 Kinase Inhibitor Improves Drug Efflux and hERG Affinity. [Abstract]2023 Dec 5;14(12):1869-1875. PMID: 38116407 -
Life Sci Alliance
Integrin β1/FAK/SRC signal pathway is involved in autism spectrum disorder in Tspan7 knockout rats. [Abstract]2022 Dec 20;6(3):e202201616. PMID: 36625203
Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Life Sci Alliance. 2022 Dec 20;6(3):e202201616. [Abstract]
Primary neurons from embryo brains of of WT rats and Tspan7−/− rats at E17 were cultured for 6 d. The WT neurons were treated without or with 10 μM Bosutinib for 4 h. Then phosphorylated and total SRC, PSD95, SYN, GluR1, and GluR2 in the primary neurons were detected with Western blot.
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PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Biochem Biophys Res Commun
Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]2020 Feb 19;522(4):862-868. PMID: 31806372 -
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Biomed Pharmacother
Interactions of bosutinib with drug transporters: In vitro and In vivo inhibition of organic cation transporter 2, multidrug and toxin extrusion protein 1, and breast cancer resistance protein by bosutinib. [Abstract]2024 Jul 24:178:117114. PMID: 39053425 -
Saudi J Biol Sci
2022 Apr;29(4):2323-2328. PMID: 35531147
Bosutinib hydrate purchased from MedChemExpress. Usage Cited in: Saudi J Biol Sci. 2022 Apr;29(4):2323-2328. [Abstract]
K562 cells were incubated with Bosutinib (BOS) (250 nM) in the absence or addition of Boc-D-FMK (5 μM) for up to 48 h. Cell cycle phase distribution was assessed using flow cytometry, PI labeling of total DNA content, and the Guava Cell Cycle Assay software module. Left to right; colored areas indicate sub-G1, G0/G1, S and G2/M phases.
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Solvent & Solubility
DMSO : 100 mg/mL (182.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Handling Instructions (2659 KB)
References
[1]. Jorge E Cortes, et al. Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial. J Clin Oncol. 2012 Oct 1;30(28):3486-92. [Content Brief]
[2]. Miriam Puttini, et al. In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res. 2006 Dec 1;66(23):11314-22. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8233 mL | 9.1164 mL | 18.2329 mL | 45.5822 mL |
| 5 mM | 0.3647 mL | 1.8233 mL | 3.6466 mL | 9.1164 mL | |
| 10 mM | 0.1823 mL | 0.9116 mL | 1.8233 mL | 4.5582 mL | |
| 15 mM | 0.1216 mL | 0.6078 mL | 1.2155 mL | 3.0388 mL | |
| 20 mM | 0.0912 mL | 0.4558 mL | 0.9116 mL | 2.2791 mL | |
| 25 mM | 0.0729 mL | 0.3647 mL | 0.7293 mL | 1.8233 mL | |
| 30 mM | 0.0608 mL | 0.3039 mL | 0.6078 mL | 1.5194 mL | |
| 40 mM | 0.0456 mL | 0.2279 mL | 0.4558 mL | 1.1396 mL | |
| 50 mM | 0.0365 mL | 0.1823 mL | 0.3647 mL | 0.9116 mL | |
| 60 mM | 0.0304 mL | 0.1519 mL | 0.3039 mL | 0.7597 mL | |
| 80 mM | 0.0228 mL | 0.1140 mL | 0.2279 mL | 0.5698 mL | |
| 100 mM | 0.0182 mL | 0.0912 mL | 0.1823 mL | 0.4558 mL |