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Documentos

SML3363

Sigma-Aldrich

GNE-317

≥98% (HPLC)

Sinônimo(s):

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

Fórmula empírica (Notação de Hill):
C19H22N6O3S
Número CAS:
1394076-92-6
Peso molecular:
414.48
Número MDL:
MFCD28900677
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

−20°C

cadeia de caracteres SMILES

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)

chave InChI

XOZLHJMDLKDZAL-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

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).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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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
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
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
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