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

Bosutinib  (Synonyms: SKI-606)

Cat. No.: HY-10158 Purity: 99.89%
COA Handling Instructions

Bosutinib is an oral 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.

Bosutinib Chemical Structure

Bosutinib Chemical Structure

CAS No. : 380843-75-4

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10 mM * 1 mL in DMSO USD 73 In-stock
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50 mg USD 132 In-stock
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200 mg USD 238 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Bosutinib:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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

IC50 & Target

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

In Vitro

Bosutinib (SKI-606) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].

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

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
Molecular Weight

530.45

Formula

C26H29Cl2N5O3

CAS No.
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)

*"≥" 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% corn oil

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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.96%

References
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Bosutinib
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