PI-103 (Hydrochloride)

PI-103 (Hydrochloride)

• CAS Number: 371935-79-4
• UNSPSC Description: PI-103 Hydrochloride is a dual 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 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy[1][2][3][4].
• Target Antigen: Apoptosis; Autophagy; DNA-PK; mTOR; PI3K
• Type: Reference compound
• Related Pathways: Apoptosis;Autophagy;Cell Cycle/DNA Damage;PI3K/Akt/mTOR
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/PI-103-Hydrochloride.html
• Purity: 98.55
• Solubility: DMSO : 4.1 mg/mL (ultrasonic;warming)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: OC1=CC(C2=NC3=C(OC4=C3C=CC=N4)C(N5CCOCC5)=N2)=CC=C1.[H]Cl
• Molecular Weight: 384.82
• References & Citations: [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):1725-38.|[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 sorafenib-treated 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 p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.cell rep methods. 2022 Jan 24;2(2):100155.|Harvard Medical School LINCS LIBRARY|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.|Cell Signal. 2024 Mar 5:118:111126.|Cell Syst. 2020 Jan 22;10(1):66-81.e11. |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.|Research Square Preprint. 2022 Jul.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: No Development Reported