Product Description: PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy[1][2][3][4].
Applications: Cancer-Kinase/protease
Formula: C19H16N4O3
Citations: Acta Biomater. 2021 Jun 1;S1742-7061(21)00357-3./Adv Funct Mater. 2021 May 24./Adv Healthc Mater. 2021 Dec 8;e2101944./Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00608-20./bioRxiv. 2024 May 31:2024.05.30.596676./BMC Cancer. 2022 Nov 24;22(1):1211./Cancer Lett. 2025 Feb 27:217532./Cell Signal. 2024 Mar 5:118:111126./Cell Syst. 2020 Jan 22;10(1):66-81.e11. /Cell Syst. 2025 Feb 26:101203./ChemMedChem. 2019 Nov 20;14(22):1933-1939./Clin Cancer Res. 2014 Nov 1;20(21):5483-95. /Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. /Exp Eye Res. 2018 Jul;172:10-20./Expert Rev Anticancer Ther. 2024 Sep 10:1-12./Front Pharmacol. 2020 Nov 11;11:580407./Harvard Medical School LINCS LIBRARY/Heliyon. 2024 May 6./J Transl Med. 2021 Dec 7;19(1):497./J Virol. 2022 Nov 23;e0145322./Molecules. 2020 Apr 23;25(8):1980./Nat Commun. 2023 Mar 28;14(1):1726./Oncogenesis. 2025 Mar 1;14(1):4./Research Square Preprint. 2022 Jul./cell rep methods. 2022 Jan 24;2(2):100155./Harvard Medical School LINCS LIBRARY
References: [1]Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39./[2]Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706./[3]López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61./[4]Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47.
CAS Number: 371935-74-9
Molecular Weight: 348.36
Compound Purity: 99.82
Research Area: Cancer
Solubility: DMSO : 10 mg/mL (ultrasonic)
Target: Apoptosis;Autophagy;DNA-PK;mTOR;PI3K
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