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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-BAY1082439
BAY1082439

Chemical Structure : BAY1082439

CAS No.: 1375469-38-7

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BAY1082439 (BAY10-82439, BAY 1082439)

货号: PC-63437Not For Human Use, Lab Use Only.

BAY1082439 is a potent, highly selective, orally available PI3Kα/β inhibitor with IC50 of 4.9 nM (PI3Kα), selectively inhibits both PI3Kα, including mutated forms of PIK3CA, and PI3Kβ in the PI3K/Akt/mTOR pathway.

规格 价格 库存 数量
10 mg ￥1380 In stock
25 mg ￥2380 In stock
50 mg ￥3980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAY1082439 is a potent, highly selective, orally available PI3Kα/β inhibitor with IC50 of 4.9 nM (PI3Kα), selectively inhibits both PI3Kα, including mutated forms of PIK3CA, and PI3Kβ in the PI3K/Akt/mTOR pathway.
BAY1082439 displays >1000-fold selectivity against mTOR kinase.
BAY1082439 induces tumor cell apoptosis and growth inhibition in PI3K-expressing and/or PTEN-driven tumor cells.
BAY1082439 is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells.
BAY1082439 effectively inhibits Pten-null prostate cancer progression

物理化学性质&存储条件

分子量 494.228
分子式 C25H30N6O5
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)-N-(8-(2-hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide

参考文献

1. Ningshu Liu, et al. Abstract 2799: BAY 1082439, a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. Abstract nr 2799. doi:1538-7445.AM2012-2799.
2. Yongkang Zou, et al. Mol Cancer Ther. 2018 Oct;17(10):2091-2099.

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