PIK-124
PIK-124 is a thiazolidinone-based PI3Kγ-biased PI3K inhibitor, with an IC50 of 3 nM against PI3Kγ. PIK-124 exhibits cross-reactivity with PI3Kα (IC50 = 23 nM), PI3Kδ (IC50 = 340 nM), PI3KC2α (IC50 = 140 nM) and PI3KC2β (IC50 = 370 nM). PIK-124 is applicable to breast cancer-related research.
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- CAS No.: 711025-68-2
- 화학식: C19H12ClFN2O3S2
- 분자량:434.88
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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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
PI3Kγ 3 nM (IC50) |
PI3Kα 23 nM (IC50) |
PI3Kδ 340 nM (IC50) |
PI3KC2α 140 nM (IC50) |
PI3KC2β 370 nM (IC50) |
In Vitro
PIK-124 shows weak inhibitory effect on p-Akt in PTEN-WT cells, but effectively inhibits PI3Kγ-enriched systems[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 711025-68-2
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분자량 434.88
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화학식 C19H12ClFN2O3S2
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SMILES
O=C1NC(=S)SC1=CC2=CC=C3OCC(=O)N(C3=C2)CC4=CC=C(F)C(Cl)=C4
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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.
Protocol
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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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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
순도&문서
References
[1]. Venable JD, et al. Phosphoinositide 3-kinase gamma (PI3Kgamma) inhibitors for the treatment of inflammation and autoimmune disease. Recent Pat Inflamm Allergy Drug Discov. 2010;4(1):1-15. [Content Brief]
[2].
Torbett NE, et al. A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition. Biochem J. 2008 Oct 1;415(1):97-110.
[Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PIK-124 Related Classifications
HY-118903 Related Classifications
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