1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. Src
    Bcr-Abl
    Autophagy
  3. Bosutinib

Bosutinib (Synonyms: SKI-606)

Cat. No.: HY-10158 Purity: 99.83%
Handling Instructions

Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.

For research use only. We do not sell to patients.

Bosutinib Chemical Structure

Bosutinib Chemical Structure

CAS No. : 380843-75-4

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200 mg USD 216 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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Description

Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.

IC50 & Target

IC50: 1.2 nM (Src), 1 nM (Abl)[1]

In Vitro

Bosutinib (100 nM; 24/48 hours) results in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N[3].
Bosutinib inhibits the proliferation of all three cell lines, with IC50s ranging from 5 nM in the KU812 line to 20 nM for the K562 and MEG-01 cell lines[3].
Bosutinib (10-500 nM; 4 hours) ablates tyrosine phosphorylation of STAT5 at 25 nM[3].

Cell Cycle Analysis[3]

Cell Line: KU812, K562 cells
Concentration: 100 nM
Incubation Time: 24 hours (KU812 cells), 48 hours (K562 cells)
Result: Resulted in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N.

Western Blot Analysis[3]

Cell Line: K562 cells
Concentration: 10 nM, 25 nM, 50 nM, 100 nM, 500 nM
Incubation Time: 4 hours
Result: Tyrosine phosphorylation of STAT5 was ablated by 25 nM.
In Vivo

Bosutinib (50-150 mg; p.o.; once a day for 5 days) remaines tumor free at 150 mg/kg, whereas at the lower doses, some relapse occurs over a 40-day period in K562 Xenografts in Nude Mice[3].

Animal Model: Nude female mice 6–7 weeks of age (K562 xenografts)[3]
Dosage: 50, 75, 100, 150 mg/kg
Administration: Oral administration, once a day for 5 days
Result: Remained tumor free at 150 mg/kg, whereas at the lower doses, some relapse occurred over a 40-day period.
Molecular Weight

530.45

Formula

C₂₆H₂₉Cl₂N₅O₃

CAS No.

380843-75-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 46 mg/mL (86.72 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8852 mL 9.4260 mL 18.8519 mL
5 mM 0.3770 mL 1.8852 mL 3.7704 mL
10 mM 0.1885 mL 0.9426 mL 1.8852 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.71 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.83%

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Bosutinib
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