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Merck
CN

SML3363

GNE-317

≥98% (HPLC)

别名:

5-(6-(3-Methoxyoxetan-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine, 5-(6-(3-Methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine, 5-[6-(3-Methoxy-3-oxetanyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-2-pyrimidinamine, GNE 317, GNE317

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关于此项目

经验公式(希尔记法):
C19H22N6O3S
化学文摘社编号:
分子量:
414.48
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

NC1=NC=C(C2=NC3=C(C(N4CCOCC4)=N2)SC(C5(COC5)OC)=C3C)C=N1

InChI

1S/C19H22N6O3S/c1-11-13-14(29-15(11)19(26-2)9-28-10-19)17(25-3-5-27-6-4-25)24-16(23-13)12-7-21-18(20)22-8-12/h7-8H,3-6,9-10H2,1-2H3,(H2,20,21,22)

InChI key

XOZLHJMDLKDZAL-UHFFFAOYSA-N

Biochem/physiol Actions

GNE-317 is an orally active potent inhibitor against phosphoinositide 3-kinase (PI3K Ki = 2/α, 27/β, 7/δ, 7/γ) and mTOR (Ki = 9 nM). GNE-317 exhibits antiproliferation potency in glioblastoma cancer cultures (EC50 from 140 to 570 nM in seven cultures) and anti-tumor efficacy in mice in vivo (40 mg/kg/d for 2 wks, then 30 mg/kg/d after; U87, GS2, and GBM10 orthotopic models).
Orally active, potent phosphoinositide 3-kinase (PI3K) and mTOR inhibitor with anti-glioblastoma efficacy in cultures in mice in vivo.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

新产品

此项目有


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Modulating the tumor microenvironment via oncolytic virus and PI3K inhibition synergistically restores immune checkpoint therapy response in PTEN-deficient glioblastoma.
Fan Xing et al.
Signal transduction and targeted therapy, 6(1), 275-275 (2021-07-29)
Ravi S Narayan et al.
Nature communications, 11(1), 2935-2935 (2020-06-12)
Personalized cancer treatments using combinations of drugs with a synergistic effect is attractive but proves to be highly challenging. Here we present an approach to uncover the efficacy of drug combinations based on the analysis of mono-drug effects. For this
Timothy P Heffron et al.
Journal of medicinal chemistry, 55(18), 8007-8020 (2012-09-06)
Inhibition of phosphoinositide 3-kinase (PI3K) signaling through PI3Kα has received significant attention for its potential in cancer therapy. While the PI3K pathway is a well-established and widely pursued target for the treatment of many cancer types due to the high
Laurent Salphati et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 18(22), 6239-6248 (2012-09-21)
Glioblastoma (GBM), the most common primary brain tumor in adults, presents a high frequency of alteration in the PI3K pathway. Our objectives were to identify a dual PI3K/mTOR inhibitor optimized to cross the blood-brain barrier (BBB) and characterize its brain
Cedric Tehranian et al.
Neuro-oncology, 24(2), 213-225 (2021-07-04)
Brain metastases (BM) are a frequent complication of malignant melanoma (MM), with limited treatment options and poor survival. Prevention of BM could be more effective and better tolerated than treating established BM in various conditions. To investigate the temporospatial dynamics

全球贸易项目编号

货号GTIN
SML3363-50MG04065268375129
SML3363-10MG04065268375112

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