PI-103 is a potent, cell-permeable, ATP-competitive PI3K family members inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110¦Á, mTORC1, PI3-KC2¦Â, p110¦Ä, mTORC2, p110¦Â, and p110¦Ã, respectively. It shows little activity against a wide array of protein kinases at 10 mM. It blocks glioma proliferation by blocking the PI 3-K/Akt pathway in vitro and in vivo. PI-103 was essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibited leukemic proliferation, the clonogenicity of leukemic progenitors and induced mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 had additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells.

June 21, 2017

prudect name : PI-103 is a potent, cell-permeable, ATP-competitive PI3K family members inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110¦Á, mTORC1, PI3-KC2¦Â, p110¦Ä, mTORC2, p110¦Â, and p110¦Ã, respectively. It shows little activity against a wide array of protein kinases at 10 mM. It blocks glioma proliferation by blocking the PI 3-K/Akt pathway in vitro and in vivo. PI-103 was essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibited leukemic proliferation, the clonogenicity of leukemic progenitors and induced mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 had additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells.
PI-103

Synonyms: CAS NO: 371935-74-9Molecular Formula: C19H16N4O3Molecular Weight: 348.36Purity: 98% minSolubility: In DMSOStorage: −20°C


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