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GDC-mTOR inhibitor

 
Catalog No.
A3637
MTOR抑制剂
组合的产品项目
规格价格库存 数量
2mg
¥ 1,758.00
Ship with 10-15 days
5mg
¥ 2,638.00
Ship with 10-15 days
10mg
¥ 3,409.00
Ship with 10-15 days
50mg
¥ 9,191.00
Ship with 10-15 days

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A

背景

Description: IC50 Value: 1.5nM (Ki) GDC-mTOR inhibitor is a potent and selective ATP-competitive inhibitor of mTOR. It's derivative drug, GDC-0349, demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. Abstract: Selective inhibitors of mammalian target of rapamycin (mTOR) kinase based upon saturated heterocycles fused to a pyrimidine core were designed and synthesized. Each series produced compounds with Ki < 10 nM for the mTOR kinase and >500-fold selectivity over closely related PI3 kinases. This potency translated into strong pathway inhibition, as measured by phosphorylation of mTOR substrate proteins and antiproliferative activity in cell lines with a constitutively active PI3K pathway. Two compounds exhibiting suitable mouse PK were profiled in in vivo tumor models and were shown to suppress mTORC1 and mTORC2 signaling for over 12 h when dosed orally. Both compounds were additionally shown to suppress tumor growth in vivo in a PC3 prostate cancer model over a 14 day study.

化学属性

StorageStore at -20°C
M.Wt474.56
Cas No.1207358-59-5
FormulaC25H30N8O2
SolubilitySoluble in DMSO
Chemical Name1-ethyl-3-[4-[4-[(3S)-3-methylmorpholin-4-yl]-7-pyrimidin-2-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea
SDFDownload SDF
Canonical SMILESCCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4=NC=CC=N4)C(=N2)N5CCOCC5C
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质量控制

质量控制和MSDS

批次:

化学结构

mTOR inhibitor