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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-SAR260301
SAR260301

Chemical Structure : SAR260301

CAS No.: 1260612-13-2

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SAR260301 (SAR-260301;SAR 260301)

货号: PC-35880Not For Human Use, Lab Use Only.

SAR260301 (SAR-260301, SAR 260301) is a potent, selective, ATP-competitive PI3Kβ inhibitor with IC50 of 52 nM in TR-FRET assays, with littile to no actiivty against PI3Kα/γ/δ (IC50=1,869/>10,000/403 nM, respectively).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SAR260301 (SAR-260301, SAR 260301) is a potent, selective, ATP-competitive PI3Kβ inhibitor with IC50 of 52 nM in TR-FRET assays, with littile to no actiivty against PI3Kα/γ/δ (IC50=1,869/>10,000/403 nM, respectively).
SAR260301 does not inhibit mTOR (IC50 >10 uM, the only other kinase inhibited by SAR260301 was VPS34 lipid kinase (IC50=180 nM) in a panel of >400 kinases.
SAR260301 inhibits AKT-Ser473 phosphorylation in cellular assays with IC50 of 32 nM, 26-fold, 88-fold, >94-fold, and >313-fold more potently than PI3Kδ, PI3Kα, PI3Kγ, and VPS34, respectively.
SAR260301 inhibits the PI3K pathway preferentially in PTEN-deficient cells, synergizes with MAPK pathway inhibitors to inhibit growth of PTEN-deficient and BRAF-mutant melanoma cells in vitro and in vivo.

物理化学性质&存储条件

分子量 354.41
分子式 C19H22N4O3
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

(S)-2-(2-(2-methylindolin-1-yl)-2-oxoethyl)-6-morpholinopyrimidin-4(1H)-one

参考文献

1. Bonnevaux H, et al. Mol Cancer Ther. 2016 Jul;15(7):1460-71.

2. Certal V, et al. J Med Chem. 2014 Feb 13;57(3):903-20.

3. Bédard PL, et al. Cancer. 2018 Jan 15;124(2):315-324.

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