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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-LY3023414
LY3023414

Chemical Structure : LY3023414

CAS No.: 1386874-06-1

LY3023414 (LY-3023414;LY 3023414)

货号: 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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5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 406.4775
分子式 C23H26N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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-

参考文献

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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