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

BCR-ABL-IN-6 (9h) 是一种选择性的 Bcr-Abl 激酶抑制剂，对 Bcr-AblWT 和 Bcr-AblT3151 的 IC50 分别为 4.6 和 227 nM。BCR-ABL-IN-6 对 Bcr-Abl 激酶具有较强的细胞内亲和力，EC50 为 14.6 nM。BCR-ABL-IN-6 是伊马替尼衍生物可用于慢性髓细胞性白血病研究的研究。

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BCR-ABL-IN-6 Chemical Structure

BCR-ABL-IN-6 Chemical Structure

CAS No. : 2499499-26-0

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BCR-ABL-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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]
细胞效力
(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]
体外研究
(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].

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

BCR-ABL-IN-6 相关抗体:

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.
体内研究
(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].

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.
分子量

505.49

Formula

C27H22F3N5O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BCR-ABL-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

BCR-ABL-IN-62499499-26-0Bcr-Abl3-Aminoindazoleethynyl linkerImatinib resistanceAntileukemicInhibitorinhibitorinhibit

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