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Merck
CN

SML2853

Sigma-Aldrich

DASA-58

≥98% (HPLC)

别名:

3-(4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-ylsulfonyl)-1,4-diazepan-1-ylsulfonyl)aniline, CID-44543605, DASA 58, DASA58, ML 203, ML-203, ML203, N,N′-DiArylSulfonAmide 58, NCGC00185916

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About This Item

经验公式(希尔记法):
C19H23N3O6S2
CAS Number:
分子量:
453.53
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

NC1=CC=CC(S(N2CCN(S(C3=CC=C(OCCO4)C4=C3)(=O)=O)CCC2)(=O)=O)=C1

InChI

1S/C19H23N3O6S2/c20-15-3-1-4-16(13-15)29(23,24)21-7-2-8-22(10-9-21)30(25,26)17-5-6-18-19(14-17)28-12-11-27-18/h1,3-6,13-14H,2,7-12,20H2

InChI key

GMHIOMMKSMSRLY-UHFFFAOYSA-N

生化/生理作用

DASA-58 is a potent and selective activator of cancer-specific pyruvate kinase isoform PKM2 (hPKM2 AC50 = 38 nM, Emax = 82%), but not PKM1, PKR or PKL, that stabilizes PKM2 tetrameric conformation by targeting a site distinct from that of fructose-1,6-bis-phosphate (FBP). DASA-58 exhibits good aqueous solubility (51.2 μg/mL), decreases cellular lactate production and suppresses cell proliferation selectively under hypoxic conditions (30 μM; H1299, 1% O2). When administered in mice, DASA-58 is reported to exhibit anti-thrombotic efficacy in vivo (40 mg/kg via iv).
Potent and selective activator of cancer-specific pyruvate kinase PKM2 in vitro and in vivo, but not PKM1, PKR or PKL.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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