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Merck
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重要文件

SML3363

Sigma-Aldrich

GNE-317

≥98% (HPLC)

同義詞:

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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About This Item

經驗公式(希爾表示法):
C19H22N6O3S
CAS號碼:
分子量::
414.48
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77
暫時無法取得訂價和供貨情況

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

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 密鑰

XOZLHJMDLKDZAL-UHFFFAOYSA-N

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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
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)
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

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