bosutinib hydrate structure
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Common Name | bosutinib hydrate | ||
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CAS Number | 918639-08-4 | Molecular Weight | 548.461 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C26H31Cl2N5O4 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of bosutinib hydrateBosutinib is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively[1]. |
Name | bosutinib hydrate |
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Synonym | More Synonyms |
Description | Bosutinib is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively[1]. |
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Related Catalog | |
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]. 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 mutantBa/F3 xenografts[2]. 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. |
References |
Molecular Formula | C26H31Cl2N5O4 |
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Molecular Weight | 548.461 |
Exact Mass | 547.175293 |
PSA | 95.34000 |
LogP | 4.42378 |
~% bosutinib hydrate CAS#:918639-08-4 |
Literature: WYETH Patent: WO2007/5462 A1, 2007 ; Location in patent: Page/Page column 15-16 ; |
~% bosutinib hydrate CAS#:918639-08-4 |
Literature: WYETH Patent: WO2007/5462 A1, 2007 ; Location in patent: Page/Page column 19-20 ; |
~% bosutinib hydrate CAS#:918639-08-4 |
Literature: WYETH Patent: WO2007/5462 A1, 2007 ; Location in patent: Page/Page column 20 ; |
SKI-606 monohydrate |
Bosulif (TN) |
4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile,hydrate |
UNII-844ZJE6I55 |
bosutinib.H2O |
Bosutinib monohydrate |
3-Quinolinecarbonitrile, 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-, hydrate (1:1) |
4-((2,4-dichloro-5-methoxyphenyl)-amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)-propoxy)-3-quinoline-carbonitrile monohydrate |
BOSULIF |
4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile hydrate (1:1) |
Bosutinib hydrate (JAN) |