Bosutinib (Synonyms: SKI-606)

Name: Bosutinib
Brand: MedChemExpress
SKU: HY-10158
Rating: 5.0 (17 reviews)

Cat. No.: HY-10158 Purity: 99.89%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 380843-75-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 238	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Bosutinib:

Bosutinib-d₈ Get quote
Bosutinib isomer Get quote
Bosutinib hydrate Get quote
Bosutinib (Standard) Get quote

17 Publications Citing Use of MCE Bosutinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Src Isoform Specific Products:

View All Isoforms

Lck Fyn Blk

Biological Activity
Purity & Documentation
References
Customer Review

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]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 10 μM Compound: SKI-606	Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay	[PMID: 16970400]
BaF3	IC₅₀	> 20 μM Compound: SKI-606	Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay	[PMID: 16970400]
BaF3	IC₅₀	0.15 μM Compound: SKI-606	Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay	[PMID: 16970400]
BaF3	IC₅₀	0.2 μM Compound: SKI-606	Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay	[PMID: 16970400]
BaF3	IC₅₀	0.2 μM Compound: SKI-606	Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay	[PMID: 16970400]
BaF3	IC₅₀	1 μM Compound: SKI-606	Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay	[PMID: 16970400]
BaF3	IC₅₀	3.2 μM Compound: Bosutinib	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay	[PMID: 26814890]
Fibroblast	IC₅₀	100 nM Compound: 1a	Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA	[PMID: 17905586]
HeLa	IC₅₀	3.85 μM Compound: Bosutinib	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
HepG2	GI₅₀	1.15 μM Compound: bosutinib, SKI-606	Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay	[PMID: 18485715]
HepG2	IC₅₀	3.91 μM Compound: bosutinib, SKI-606	Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay	[PMID: 18485715]
HT-29	GI₅₀	1.17 μM Compound: bosutinib, SKI-606	Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay	[PMID: 18485715]
HT-29	IC₅₀	3.87 μM Compound: bosutinib, SKI-606	Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay	[PMID: 18485715]
K562	IC₅₀	0.0043 μM Compound: Bosutinib	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26814890]

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.

380843-75-4

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 year; -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
10 mM	0.1885 mL	0.9426 mL	1.8852 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 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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 year; -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%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (250 KB) HNMR (180 KB) LCMS (104 KB)

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

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

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.

Keywords:

Bosutinib380843-75-4SKI-606SKI606SKI 606SrcBcr-AblAutophagyOralSrc/Abl tyrosine kinase inhibitorcancerInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Bosutinib (Synonyms: SKI-606)

Customer Review

Other Forms of Bosutinib:

Bosutinib Related Antibodies

17 Publications Citing Use of MCE Bosutinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Src Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Bosutinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Bosutinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report