Art. -Nr.: HY-10158A

Bosutinib hydrate

(Synonyms: SKI-606 hydrate)

24 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.97%
CAS. Nr.: 918639-08-4
Formel: C₂₆H₃₁Cl₂N₅O₄
Molecular Weight:548.46

Speicherung:

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)

Bosutinib hydrate Chemical Structure

CAS. Nr.: 918639-08-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC₅₀ of 1.2 nM and 1 nM, respectively^[1].

IC₅₀ & Target

IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).

Alle Src Isoform-spezifische Produkte anzeigen :

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

In Vitro

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.

Cell Proliferation Assay^[2]

Cell Line:

The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)
Concentration:

0.1 μmol/L
Incubation Time:

72 h
Result:

Inhibited several human CML derived cell lines with IC₅₀ values ranging from 1 to 20 nmol/L.

In Vivo

Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) hydrate has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) hydrate has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

KU812CM L xenograft model^[2]
Dosage:

75 mg/kg twice daily or 150 mg/kg once daily
Administration:

Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily)
Result:

Had the therapeutic activity and produced a dose- and schedule-dependent weight loss.

Animal Model:

Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts^[2]
Dosage:

150 mg/kg
Administration:

Bosutinib (150 mg/kg; once daily, 5 days weekly)
Result:

Decreased the rate of tumor growth and prolonged event-free survival of mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 918639-08-4
Appearance Solid
Molecular Weight 548.46
Formel C₂₆H₃₁Cl₂N₅O₄
Color White to off-white
SMILES

CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC.O
Synonyms

SKI-606 hydrate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

All Cell Imaging/StainingWBFlow CytometryCell Proliferation/Viability AssayHistological Imaging/Staining

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Journal Impact Factor

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

SRC kinase drives multidrug resistance induced by KRAS-G12C inhibition. [Abstract]

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.
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

Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1. [Abstract]

2021 Mar 8;12:644342. PMID: 33790797
ACS Omega

Discovery of PLpro and Mpro Inhibitors for SARS-CoV-2. [Abstract]

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.
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
bioRxiv

2025 February 26.
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

Protective effect of Bosutinib with caspase inhibitors on human K562 cells. [Abstract]

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.
Technical University of Munich

24.01.2018.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8233 mL

9.1164 mL

18.2329 mL

5 mM

0.3647 mL

1.8233 mL

3.6466 mL

10 mM

0.1823 mL

0.9116 mL

1.8233 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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

Keywords

Bosutinib hydrate

24 Cited Publications

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Bosutinib hydrate

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Publications Citing Use of MedChemExpress (MCE) Bosutinib hydrate

Alle Src Isoform-spezifische Produkte anzeigen

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bosutinib hydrate Related Classifications

HY-10158A Related Classifications