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

Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor 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
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Based on 16 publication(s) in Google Scholar

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Description

Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor 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].

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) 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].

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
Molecular Weight

530.45

Formula

C26H29Cl2N5O3

CAS No.
Appearance

Solid

Color

White to yellow

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, 1 years; -20°C, 6 months (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 46 mg/mL (86.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the 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, 1 years; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.96%

References

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, 1 years; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8852 mL 9.4260 mL 18.8519 mL 47.1298 mL
5 mM 0.3770 mL 1.8852 mL 3.7704 mL 9.4260 mL
10 mM 0.1885 mL 0.9426 mL 1.8852 mL 4.7130 mL
15 mM 0.1257 mL 0.6284 mL 1.2568 mL 3.1420 mL
20 mM 0.0943 mL 0.4713 mL 0.9426 mL 2.3565 mL
25 mM 0.0754 mL 0.3770 mL 0.7541 mL 1.8852 mL
30 mM 0.0628 mL 0.3142 mL 0.6284 mL 1.5710 mL
40 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1782 mL
50 mM 0.0377 mL 0.1885 mL 0.3770 mL 0.9426 mL
60 mM 0.0314 mL 0.1571 mL 0.3142 mL 0.7855 mL
80 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5891 mL
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Bosutinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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