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Bosutinib

SKU: orb1225150

Description

Bosutinib is a Bcr-Abl kinase inhibitor for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Compared to other tyrosine kinase inhibitors, it has a more favourable hematologic toxicity profile. FDA approved on September 4, 2012. (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.(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.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Bosutinib

Key Properties

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CAS Number380843-75-4
MW530.45
Purity>98% (HPLC)
FormulaC26H29Cl2N5O3
SMILESN#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=C1
TargetBcr-Abl
SolubilityEthanol: 2 mg/mL (3.77 mM); DMSO: 100 mg/mL (188.51 mM)

Bioactivity

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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. Animal model: KU812CM L xenograft model. 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. 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.
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. Cell Proliferation Assay 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

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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SKI 606

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Quick Database Links

Gene Symbol
Bcr-Abl

Protocol Information

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