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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)

Formulário

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).
Orally active, potent phosphoinositide 3-kinase (PI3K) and mTOR inhibitor with anti-glioblastoma efficacy in cultures in mice in vivo.

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

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Certificados de análise (COA)

Lot/Batch Number

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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
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
Laurent Salphati et al.
Drug metabolism and disposition: the biological fate of chemicals, 42(7), 1110-1116 (2014-04-24)
Glioblastoma multiforme (GBM) is the most common primary brain tumor in adults, and the limited available treatment options have not meaningfully impacted patient survival in the past decades. Such poor outcomes can be at least partly attributed to the inability

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