Bosutinib hydrate

SKU: orb1940870

Description

Bosutinib (hydrate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range.IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).

Images & Validation

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Key Properties

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CAS Number	918639-08-4
MW	548.46
Purity	>98% (HPLC)
Formula	C₂₆H₃₁Cl₂N₅O₄
SMILES	CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC.O
Solubility	In Vitro: DMSO : 100 mg/mL (182.33 mM)

Bioactivity

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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. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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