1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl
  3. BCR-ABL-IN-6

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.

For research use only. We do not sell to patients.

BCR-ABL-IN-6 Chemical Structure

BCR-ABL-IN-6 Chemical Structure

CAS No. : 2499499-26-0

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Description

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[1]. 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.

IC50 & Target

IC50: 4.6 nM (Bcr-AblWT), 227 nM (Bcr-AblT3151)[1]

In Vitro

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[1].
BCR-ABL-IN-6 (10 μM; 1 h) suppresses Bcr-Abl phosphorylation dose dependenly and results underscored selective antiproliferative effects towards Bcr-Abl [1].
BCR-ABL-IN-6 (10 μM; 1 h) shows great selectivity cytotoxic between K562 and L132 cells[1].
BCR-ABL-IN-6 (10 μM) shows strong cytostatic activity against K562 and HL60 cells[1].
BCR-ABL-IN-6 (10 μM) shows exceptional selective antiproliferative effects towards the Bcr-Abl positive leukemia cell K562[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: K562 cell line
Concentration: 0.003, 0.01, 0.03, 0.1 and 0.3 μM
Incubation Time: 1 h
Result: Showed a dose-dependent suppression of Bcr-Abl phosphorylation.

Cell Viability Assay[1]

Cell Line: K562 and L132 cell lines
Concentration: 10 μM
Incubation Time: 1 h
Result: Exerted cellular activity with GI50 less than 160 nM against the Bcr-Abl positive leukemia K562 cells and exerted superior cellular potencies to imatinib with GI50 of 0.02 μM. Showed selectivity cytotoxic effects to the normal cell L132 with GI50 of 9.27 μM.
In Vivo

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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice[1]
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.
Molecular Weight

505.49

Formula

C27H22F3N5O2

CAS No.
SMILES

O=C(NC1=CC=CC(C#CC2=CC=CC3=C2C(N)=NN3)=C1)C4=CC=C(N5CCOCC5)C(C(F)(F)F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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BCR-ABL-IN-6 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BCR-ABL-IN-6
Cat. No.:
HY-150569
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