SML3959

VS-5584

≥98% (HPLC)

• Sinonimo/i: 5-(9-Isopropyl-8-methyl-2-morpholin-4-yl-9H-purin-6-yl)-pyrimidin-2-ylamine, 5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine, SB 2343, SB-2343, SB2343, VS 5584, VS5584
• Formula empirica (notazione di Hill): C₁₇H₂₂N₈O
• Numero CAS: 1246560-33-7
• Peso molecolare: 354.41
• Numero MDL: MFCD25372027
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear
• Temperatura di conservazione: -10 to -25°C
• Stringa SMILE: N4(CCOCC4)c1nc2[n](c(nc2c(n1)c3cnc(nc3)N)C)C(C)C
• InChI: QYBGBLQCOOISAR-UHFFFAOYSA-N

Descrizione

Azioni biochim/fisiol

Orally active, potent and highly selective mTOR and class I phosphoinositide 3-kinases (PI 3-kinases; PI3K) inhibitor with anti-cancer efficacy in vitro and in vivo.


VS-5584 (SB2343) is an orally active, potent and highly selective mTOR (IC50 = 37 nM) and class I phosphoinositide 3-kinases (PI 3-kinases; PI3K IC50 = 16 nM/α, 68 nM/β, 25 nM/γ, 42 nM/δ; little activity toward 400 other lipid and protein kinases) inhibitor with broad-spectrum anti-proliferation activity in cancer cultures (IC50 post 48h treatment from 48 nM to 1.75 μM among 50 cancer lines) by inhibiting PI3K and mTOR downstream substrates phosphorylation. VS-5584 displays tumor growth inhibition efficacy in various rapalog-sensitive and -resistant human xenograft models in mice in vivo (PC3 TGI = 79% and 113%, respectively, post 28-day 11 mg/kg or 25 mg/kg daily p.o. treatment).

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable