SML4203

VVD-133214

≥98% (HPLC)

• Synonim(y): (S,E)-N-(1-Cyclopropyl-3-(methylsulfonyl)allyl)-2-(1,1-difluoroethyl)-4-phenoxypyrimidine-5-carboxamide, 5-Pyrimidinecarboxamide, N-[(1S,2E)-1-cyclopropyl-3-(methylsulfonyl)-2-propen-1-yl]-2-(1,1-difluoroethyl)-4-phenoxy- (ACI), RO 7589831, RO-7589831, RO7589831, VVD 133214, VVD 214, VVD-214, VVD133214, VVD214
• Wzór empiryczny (zapis Hilla): C₂₀H₂₁F₂N₃O₄S
• Numer CAS: 3026500-20-6
• Masa cząsteczkowa: 437.46
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: protect from light

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• storage condition: protect from light
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Opis

Biochem/physiol Actions

VVD-133214 (RO7589831, VVD214) is an orally active, allosteric WRN inhibitor that covalently targets helicase domain Cys727 (hWRN(519-1227) DNA unwinding IC50 = 130 nM with and 1.3 μM without ATP preincubation). VVD214 binds WRN in a nucleotide-cooperative manner, causing widespread double-stranded DNA breaks, nuclear swelling and cell death in cells with high microsatellite instability (MSI-high, MSI-H; HCT-116 GI50 = 66 nM), but not in microsatellite-stable (MSS) cells (SW480 GI50 > 20 μM). VVD214 causes tumour regression in multiple MSI-H colorectal cancer cell lines-derived and patient-derived xenograft models in vivo (20 mg/kg via daily p.o.).

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable