LY-3023414 - CAS 1386874-06-1
Catalog number: 1386874-06-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C23H25N4O3
Molecular Weight:
406.48
COA:
Inquire
Targets:
Akt | PI3K
Description:
LY3023414, a quinoline derivative, has been found to be a PI3Kα and mTOR inhibitor that could influence cell proliferation and cycle of tumor cells. It was just planed a Phase II trial for Pancreatic cancer by Eli Lilly.
Purity:
98%
Appearance:
Powder
Synonyms:
LY3023414; UNII-C88817F47Y; LY-3023414; C88817F47Y; GTPL8918; 8-[5-(2-hydroxypropan-2-yl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methylimidazo[4,5-c]quinolin-2-one
Solubility:
10 mM in DMSO
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
LY3023414 has been found to be a PI3Kα and mTOR inhibitor that could influence cell proliferation and cycle of tumor cells.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
ACCFLVVUVBJNGT-AWEZNQCLSA-N
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
Canonical SMILES:
CC(CN1C2=C3C=C(C=CC3=NC=C2N(C1=O)C)C4=CC(=CN=C4)C(C)(C)O)OC
Current Developer:
Eli Lilly; Memorial Sloan-Kettering Cancer Center
1.Dual PI3K/mTOR Inhibition in Colorectal Cancers with
Foley TM;Payne SN;Pasch CA;Yueh AE;Van De Hey DR;Korkos DP;Clipson L;Maher ME;Matkowskyj KA;Newton MA;Deming DA Mol Cancer Res. 2017 Feb 9;15(3):317-327. doi: 10.1158/1541-7786.MCR-16-0256. [Epub ahead of print]
Therapeutic targeting of the PI3K pathway is an active area of research in multiple cancer types, including breast and endometrial cancers. This pathway is commonly altered in cancer and plays an integral role in numerous vital cellular functions. Mutations in the ;PIK3CA; gene, resulting in a constitutively active form of PI3K, often occur in colorectal cancer, though the population of patients who would benefit from targeting this pathway has yet to be identified. In human colorectal cancers, ;PIK3CA; mutations most commonly occur concomitantly with loss of adenomatous polyposis coli (APC). Here, treatment strategies are investigated that target the PI3K pathway in colon cancers with mutations in ;APC; and ;PIK3CA; Colorectal cancer spheroids with ;Apc; and ;Pik3ca; mutations were generated and characterized confirming that these cultures represent the tumors from which they were derived. Pan and alpha isomer-specific PI3K inhibitors did not induce a significant treatment response, whereas the dual PI3K/mTOR inhibitors BEZ235 and LY3023414 induced a dramatic treatment response through decreased cellular proliferation and increased differentiation. The significant treatment responses were confirmed in mice with ;Apc; and ;Pik3ca;-mutant colon cancers as measured using endoscopy with a reduction in median lumen occlusion of 53% with BEZ235 and a 24% reduction with LY3023414 compared with an increase of 53% in controls (;P; < 0.
2.PI3K-mTOR pathway identified as a potential therapeutic target in biliary tract cancer using a newly established patient-derived cell panel assay.
Sakamoto Y;Yamagishi S;Tanizawa Y;Tajimi M;Okusaka T;Ojima H Jpn J Clin Oncol. 2018 Apr 1;48(4):396-399. doi: 10.1093/jjco/hyy011.
Biliary tract carcinoma (BTC) is an extremely malignant tumor, but available treatment options are limited. Despite of needs for novel therapies, few BTC-related resources are currently available for evaluation of candidate drugs. To address this issue, we have recently established 13 cell lines from surgical specimens from Japanese BTC patients. In the present study, we evaluated four new molecular targeting agents using our BTC cell-based assay panel with 17 BTC cell lines. PI3K/mTOR dual inhibitor LY3023414 showed activity at submicromolar concentration ranges against 13 of the 17 cell lines tested, including the ones with gemcitabine insensitivity. In conclusion, we demonstrated that in vitro study with the BTC cell line panel would be an efficient approach to screen for novel therapeutic strategies. Although this is preliminary result and further investigations are required for confirmation, PI3K/mTOR inhibitor might be a potential target for BTC drug development.
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