SML1762

SI-2

≥98% (HPLC)

• Synonyme(s) : (1E)-1-(2-Pyridinyl)ethanone 1-(1-methyl-1H-benzoimidazol-2-yl)-hydrazone, (1E)-N-(1-Methyl-1H-benzoimidazol-2-yl)-N′-(1-pyridin-2-yl-ethylidene)-hydrazine
• Formule empirique (notation de Hill): C₁₅H₁₅N₅
• Numéro CAS: 380537-35-9
• Poids moléculaire : 265.31
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: , light yellow to dark orange
• Solubilité: DMSO: 20 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: C/C(C1=CC=CC=N1)=N\NC2=NC3=C(C=CC=C3)N2C

Description

Actions biochimiques/physiologiques

SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity (Effec. conc. >/= 5 nM in cell-based SRC-1, SRC-2, and SRC-3 reporter assays) by downregulating SRCs protein, but not transcript level (Effec. conc. >/= 12.5 nM against SRC-3, >/= 25 nM against SRC-1 and SCR-2 in MDA-MB-468 culture). SI-2 is cytotoxic to breast cancer cultures (IC₅₀ = 1.5 nM/BT-474, 3.4 nM/MDA-MB-468, 22 nM/MCF-7), but not to normal hepatocytes even at 500 nM concentration. SI-2 is reported to be orally available in mice and, when administered intraperitoneally (2 mg/kg b.i.d.), effectively suppress MDA-MB-468-derived tumor expansion in mice in vivowith good pharmacokinetics (C_max = 30 μM, t_max = 0.25 h, t_1/2 = 1.0 h; 20 mg/kg i.p.) and no apparent adverse effects to the animals.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H315,H319
• Conseils de prudence: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• Classification des risques: Eye Irrit. 2 - Skin Irrit. 2
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable