产品
编 号：F753413
分子式：C27H22F3N5O2
分子量：505.49
分子式：C27H22F3N5O2
分子量：505.49
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CAS No: 2499499-26-0
产品详情
生物活性：
BCR-ABL-IN-6 (9h) is a selective Bcr-Abl kinase inhibitor with IC50s of 4.6 and 227 nM for Bcr-AblWT and Bcr-AblT3151 respectively. BCR-ABL-IN-6 inhibits Bcr-Abl kinase with strong affinity inside the cells with an EC50 of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia. BCR-ABL-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
BCR-ABL-IN-6 (5 and 10 mg/kg; male ICR mice; for 9 h) takes 0.6 h to reach the maximum concentration (Cmax). With intravenous and oral administration, the AUClast values of BCR-ABL-IN-6 are 14018.7 ng·h/mL and 174.7 ng·h/mL. BCR-ABL-IN-6 intravenous administration is better, but unfavorable oral administration.Animal Model:Male ICR mice
Dosage:5 mg/kg and 10 mg/kg
Administration:Intravenous and oral; 5 and 10 mg/kg; for 9h
Result:Oral administration is not as effective as intravenous injection, intravenous injection is better.
体外研究：
BCR-ABL-IN-6(10 μM; 1 h) againts with c-Src which is a closely related kinase domain of Bcr-Abl and exerts superior cellular potencies to imatinib.BCR-ABL-IN-6 (10 μM; 1 h) suppresses Bcr-Abl phosphorylation dose dependenly and results underscored selective antiproliferative effects towards Bcr-Abl . BCR-ABL-IN-6 (10 μM; 1 h) shows great selectivity cytotoxic between K562 and L132 cells.BCR-ABL-IN-6 (10 μM) shows strong cytostatic activity against K562 and HL60 cells.BCR-ABL-IN-6 (10 μM) shows exceptional selective antiproliferative effects towards the Bcr-Abl positive leukemia cell K562.
BCR-ABL-IN-6 (9h) is a selective Bcr-Abl kinase inhibitor with IC50s of 4.6 and 227 nM for Bcr-AblWT and Bcr-AblT3151 respectively. BCR-ABL-IN-6 inhibits Bcr-Abl kinase with strong affinity inside the cells with an EC50 of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia. BCR-ABL-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
BCR-ABL-IN-6 (5 and 10 mg/kg; male ICR mice; for 9 h) takes 0.6 h to reach the maximum concentration (Cmax). With intravenous and oral administration, the AUClast values of BCR-ABL-IN-6 are 14018.7 ng·h/mL and 174.7 ng·h/mL. BCR-ABL-IN-6 intravenous administration is better, but unfavorable oral administration.Animal Model:Male ICR mice
Dosage:5 mg/kg and 10 mg/kg
Administration:Intravenous and oral; 5 and 10 mg/kg; for 9h
Result:Oral administration is not as effective as intravenous injection, intravenous injection is better.
体外研究：
BCR-ABL-IN-6(10 μM; 1 h) againts with c-Src which is a closely related kinase domain of Bcr-Abl and exerts superior cellular potencies to imatinib.BCR-ABL-IN-6 (10 μM; 1 h) suppresses Bcr-Abl phosphorylation dose dependenly and results underscored selective antiproliferative effects towards Bcr-Abl . BCR-ABL-IN-6 (10 μM; 1 h) shows great selectivity cytotoxic between K562 and L132 cells.BCR-ABL-IN-6 (10 μM) shows strong cytostatic activity against K562 and HL60 cells.BCR-ABL-IN-6 (10 μM) shows exceptional selective antiproliferative effects towards the Bcr-Abl positive leukemia cell K562.
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