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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2499499-26-0
分子式: C₂₇H₂₂F₃N₅O₂
分子量:505.49

保管条件:

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

Data Sheet (275 KB)

BCR-ABL-IN-6 構造式

CAS 番号: 2499499-26-0

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

Related Protocols :

EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)

化学情報

CAS 番号 2499499-26-0
分子量 505.49
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (275 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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