711025-68-2
Chemical Structure
PIK-124
- CAS No.: 711025-68-2
- Formula:C19H12ClFN2O3S2
- Molecular Weight:434.88
IUPAC Name: (E)-4-(3-chloro-4-fluorobenzyl)-6-((4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-2H-benzo[b][1,4]oxazin-3(4H)-one
InChIKey: KWDKVVZOYYHCRG-FRKPEAEDSA-N
SMILES: O=C1NC(=S)SC1=CC2=CC=C3OCC(=O)N(C3=C2)CC4=CC=C(F)C(Cl)=C4
Biological Activity: 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[1][2].
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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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- [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]
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[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]
Keywords
