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LY3023414

Chemical Structure : LY3023414

CAS No.: 1386874-06-1

LY3023414 (LY-3023414;LY 3023414)

Catalog No.: PC-43082Not For Human Use, Lab Use Only.

LY3023414 is a potent, dual PI3K/mTOR inhibitor with IC50 of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 165 nM and 4.24 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTOR and DNA-PK, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LY3023414 is a potent, dual PI3K/mTOR inhibitor with IC50 of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 165 nM and 4.24 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTOR and DNA-PK, respectively.
LY3023414 inhibits the phosphorylation of AKT at position T308 with IC50 of 106 nM in the PTEN-deficient U87 MG glioblastoma cell line, inhibits phosphorylation of AKT at position S473 (IC50=94.2 nM) by mTORC2 as well as phosphorylation of mTORC1 kinase targets p70S6K (position T389; IC50=10.6 nM).
LY3023414 causes G1 cell-cycle arrest and shows broad antiproliferative activity in cancer cell panel screens.
LY3023414 exhibits antitumor activity in multiple xenograft models.

Physicochemical Properties

M.Wt 406.4775
Formula C23H26N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2H-Imidazo[4,5-c]quinolin-2-one, 1,3-dihydro-8-[5-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(2S)-2-methoxypropyl]-3-methyl-

References

1. Smith MC, et al. Mol Cancer Ther. 2016 Oct;15(10):2344-2356.

2. Zaidi AH, et al. Ann Surg. 2017 Jul;266(1):91-98.

3. Wei L, et al. Oncotarget. 2016 Nov 22;7(47):76374-76389.

4. Zheng L, et al. Oncotarget. 2017 Oct 27;8(58):98964-98973.

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