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Cat. No.: HY-150569

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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-Abl^WT and Bcr-Abl^T3151 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.

CAS No.: 2499499-26-0
Formula: C₂₇H₂₂F₃N₅O₂
Molecular Weight:505.49

Storage:

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

Data Sheet (275 KB)

BCR-ABL-IN-6 Chemical Structure

CAS No.: 2499499-26-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

BCR-ABL-IN-6 (9h) is a selective Bcr-Abl kinase inhibitor with IC₅₀s of 4.6 and 227 nM for Bcr-Abl^WT and Bcr-Abl^T3151 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-Abl^WT), 227 nM (Bcr-Abl^T3151)^[1]

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	GI₅₀	1.36 μM Compound: 9h	Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32961435]
HL-60(TB)	GI₅₀	1.4 μM Compound: 9h	Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32961435]
K562	GI₅₀	<0.01 μM Compound: 9h	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32961435]
K562	GI₅₀	0.02 μM Compound: 9h	Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32961435]
L132	GI₅₀	9.27 μM Compound: 9h	Antiproliferative activity against human L132 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human L132 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32961435]
MOLT-4	GI₅₀	1.31 μM Compound: 9h	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32961435]
RPMI-8226	GI₅₀	1.98 μM Compound: 9h	Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32961435]
SR	GI₅₀	2.4 μM Compound: 9h	Antiproliferative activity against human SR cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SR cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32961435]

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 (C_max). With intravenous and oral administration, the AUC_last 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.

Chemical Information

CAS No. 2499499-26-0
Molecular Weight 505.49
Formula C₂₇H₂₂F₃N₅O₂
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. El-Damasy AK, et al. Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity[J]. European Journal of Medicinal Chemistry, 2020, 207:112710. [Content Brief]

[2]. El-Damasy AK, et al. Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity[J]. European Journal of Medicinal Chemistry, 2020, 207:112710. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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BCR-ABL-IN-6

All Bcr-Abl Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

BCR-ABL-IN-6 Related Classifications

HY-150569 Related Classifications