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MilliporeSigma

SML4203

VVD-133214

≥98% (HPLC)

Synonym(s):

(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

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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
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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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