LY3023414

• CAT Number: I001489
• CAS Number: 1386874-06-1
• Molecular Formula: C23H26N4O3
• Molecular Weight: 406.48
• Purity: ≥95%
• Target: PI3K
• Solubility: 10 mM in DMSO
• Storage: Store at -20℃
• IUPAC Name: 8-[5-(2-hydroxypropan-2-yl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methylimidazo[4,5-c]quinolin-2-one
• InChI: InChI=1S/C23H26N4O3/c1-14(30-5)13-27-21-18-9-15(16-8-17(11-24-10-16)23(2,3)29)6-7-19(18)25-12-20(21)26(4)22(27)28/h6-12,14,29H,13H2,1-5H3/t14-/m0/s1
• InChIKey: ACCFLVVUVBJNGT-AWEZNQCLSA-N
• SMILES: CC(CN1C2=C3C=C(C=CC3=NC=C2N(C1=O)C)C4=CC(=CN=C4)C(C)(C)O)OC

LY3023414 (Cat.No:I001489) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).

Reference

1:PI3K/mTOR Dual Inhibitor, LY3023414, Demonstrates Potent Antitumor Efficacy Against Esophageal Adenocarcinoma in a Rat Model. Zaidi AH, Kosovec JE, Matsui D, Omstead AN, Raj M, Rao RR, Biederman RW, Finley GG, Landreneau RJ, Kelly RJ, Jobe BA.Ann Surg. 2016 Jul 29. [Epub ahead of print] PMID: 27471841 2:Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth. Smith MC, Mader MM, Cook JA, Iversen P, Ajamie R, Perkins E, Bloem L, Yip YY, Barda DA, Waid PP, Zeckner DJ, Young DA, Sanchez-Felix M, Donoho GP, Wacheck V.Mol Cancer Ther. 2016 Oct;15(10):2344-2356. Epub 2016 Jul 20. PMID: 27439478