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SML3824

Sigma-Aldrich

DRB18

new

≥98% (HPLC)

Sinônimo(s):

5,5′-(((4-Chloro-1,2-phenylene)bis(azanediyl))bis(methylene))bis(2-methylphenol), DRB 18, DRB-18

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About This Item

Fórmula empírica (Notação de Hill):
C22H23ClN2O2
Número CAS:
Peso molecular:
382.88
Número MDL:
Código UNSPSC:
12352200

Nível de qualidade

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

-10 to -25°C

cadeia de caracteres SMILES

ClC1=CC=C(C(NCC2=CC=C(C)C(O)=C2)=C1)NCC3=CC=C(C)C(O)=C3

Ações bioquímicas/fisiológicas

Class I glucose transporters (GLUT1-4) inhibitor with greater anti-cancer efficacy than WZB117 (WZB-117) in cultures and in vivo.



DRB18 is a class I glucose transporters (GLUT1-4) inhibitor (glucose uptake IC50 = 2.6/8.8/4.5/0.9 µM using HEK293 GLUT1/2/3/4 transfectants) that exhibits greater anti-cancer efficacy than WZB117 (WZB-117) in cultures (IC50 <10 µM in 51 of 60 cancer cultures tested vs. only 17 from the same 60 cultures when using WZB117) and suppresses A549 xenografts-derived tumor growth in mice in vivo (44% reduction with 10 mg/kg i.p. 3x per wk for 5 wks) by altering the abundance of metabolites in glucose-related pathways.

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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Amanda Westergren Jakobsson et al.
Cancers, 14(13) (2022-07-10)
Neuroblastoma, the most common solid tumor in children, is characterized by amplification of the MYCN proto-oncogene, a high-risk aggressive clinical marker associated with treatment failure. MYCN plays an important role in cell growth, proliferation, metabolism, and chemoresistance. Here, we show
Pratik Shriwas et al.
Cancer & metabolism, 9(1), 14-14 (2021-03-28)
Cancer cells drastically increase the uptake of glucose and glucose metabolism by overexpressing class I glucose transporters (GLUT1-4) to meet their energy and biomass synthesis needs and are very sensitive and vulnerable to glucose deprivation. Although targeting glucose uptake via
Qingzhu Shi et al.
Cancer cell, 40(10), 1207-1222 (2022-09-10)
How glucose metabolism remodels pro-tumor functions of tumor-associated macrophages (TAMs) needs further investigation. Here we show that M2-like TAMs bear the highest individual capacity to take up intratumoral glucose. Their increased glucose uptake fuels hexosamine biosynthetic pathway-dependent O-GlcNAcylation to promote

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