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Merck
CN

SML3824

DRB18

≥98% (HPLC)

别名:

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

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关于此项目

经验公式(希尔记法):
C22H23ClN2O2
化学文摘社编号:
分子量:
382.88
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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InChI

1S/C22H23ClN2O2/c1-14-3-5-16(9-21(14)26)12-24-19-8-7-18(23)11-20(19)25-13-17-6-4-15(2)22(27)10-17/h3-11,24-27H,12-13H2,1-2H3

InChI key

WNTAQMQIZGJASL-UHFFFAOYSA-N

SMILES string

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

Biochem/physiol Actions

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.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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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
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
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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