SML2853

DASA-58

≥98% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₉H₂₃N₃O₆S₂
• CAS-Nummer: 1203494-49-8
• Molekulargewicht: 453.53
• MDL-Nummer: MFCD29472280
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: 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
• InChIKey: GMHIOMMKSMSRLY-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

DASA-58 is a potent and selective activator of cancer-specific pyruvate kinase isoform PKM2 (hPKM2 AC50 = 38 nM, E_max = 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).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable