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About This Item
Empirical Formula (Hill Notation):
C20H21F2N3O4S
CAS Number:
Molecular Weight:
437.46
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
protect from light
Quality Segment
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
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.).
Storage Class
11 - Combustible Solids
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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