Bosutinib hydrate
CAS No. 918639-08-4
Bosutinib hydrate( —— )
Catalog No. M25044 CAS No. 918639-08-4
Bosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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Biological Information
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Product NameBosutinib hydrate
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NoteResearch use only, not for human use.
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Brief DescriptionBosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
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DescriptionBosutinib (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).
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In VitroBosutinib (hydrate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range.Cell Proliferation AssayCell Line:The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)Concentration:0.1 μmol/LIncubation Time:72 hResult:Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L.
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In VivoBosutinib (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 dailyAdministration: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 xenograftsDosage: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.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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Recptor——
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Research Area——
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Indication——
Chemical Information
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CAS Number918639-08-4
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Formula Weight548.46
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Molecular FormulaC26H31Cl2N5O4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (182.33 mM)
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SMILESCN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC.O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.
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.
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