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

Bosutinib hydrate  (Synonyms: SKI-606 hydrate)

Cat. No.: HY-10158A Purity: 99.87%
SDS COA Handling Instructions

Bosutinib (hydrate) 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 hydrate Chemical Structure

Bosutinib hydrate Chemical Structure

CAS No. : 918639-08-4

Size Price Stock Quantity
5 mg USD 42 In-stock
10 mg USD 66 In-stock
50 mg USD 132 In-stock
100 mg USD 198 In-stock
200 mg USD 238 In-stock
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Based on 17 publication(s) in Google Scholar

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Description

Bosutinib (hydrate) is an oral 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).

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 (hydrate) (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (hydrate) (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

548.46

Formula

C26H31Cl2N5O4

CAS No.
Appearance

Solid

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

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 : 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8233 mL 9.1164 mL 18.2329 mL
5 mM 0.3647 mL 1.8233 mL 3.6466 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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
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Bosutinib hydrate 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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Bosutinib hydrate
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HY-10158A
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