Ack1 inhibitor 1
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity.
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- CAS No.: 2924415-92-7
- 화학식: C39H40F3N7O4
- 분자량:727.77
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| NCI-H1975 | IC50 |
4.18 nM
Compound: 10zi
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Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by SRB colorimetric assay
Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by SRB colorimetric assay
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[PMID: 37134203] |
In Vitro
Ack1 inhibitor 1 inhibits of cell growth with IC50s of 3.71 μM and 4.18 μM in 67R and H1975 cells[1].
Ack1 inhibitor 1 (0 nM-5000 nM, 72 h) alone or in combination with ASK120067 enhances antitumor effects in 67R[1].
Ack1 inhibitor 1 (1 μM and 5 μM, 6 h) inhibits the phosphorylation of ACK1 and AKT in 67R cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:67R cells (ASK120067-resistant cells obtained from parental H1975 cells by a dose escalation method).
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Concentration:0-5000 nM (combined with ASK120067)
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Incubation Time:72 h
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Result:Caused strong synergistic anti-growth effects on 67R cells with high synergy scores of 10.83, respectively
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Cell Line:67R cells
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Concentration:1 μM and 5 μM
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Incubation Time:6 h (stimulated with or without EGF for 30 min)
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Result:Caused moderate down-regulation of p-ACK1 and p-AKT at 1 μM.
Exhibited better potency against p-AKT, while it was unable to completely inhibit p-ACK1 at 5 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2924415-92-7
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분자량 727.77
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화학식 C39H40F3N7O4
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SMILES
CN(CC1)CCN1C(C=C2)=CC(OCC)=C2NC3=NC=C4C(N(C[C@@H]5OCCC5)C(C(C6=CC(NC(C7=CC(C(F)(F)F)=CC=C7)=O)=CC=C6)=C4)=O)=N3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
In Vivo:
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Protocol
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ack1 inhibitor 1 Related Classifications
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