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VVD-214

Cat. No. 9027 Submit a Review Datasheet / COA / SDS
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Description: Potent WRN covalent allosteric inhibitor; orally bioavailable
Alternative Names: RO7589831
Chemical Name: N-[(1S,2E)-1-Cyclopropyl-3-(methylsulfonyl)-2-propen-1-yl]-2-(1,1-difluoroethyl)-4-phenoxy-5-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for VVD-214

VVD-214 is a potent werner syndrome helicase (WRN) covalent allosteric inhibitor (IC50 = 0.13 μM and 2.4 μM with and without ATP, respectively). The selective binding of VVD-214 to cysteine C727 of WRN triggers double-stranded DNA breaks, nuclear swellings, cell death and tumor regression in microsatellite instability-high (MSI-H) colorectal cancer models. Highly stable in hepatocytes and whole blood, VVD-214 is orally bioavailable.

Licensing Information

Sold with permission from Vividion Therapeutics

Technical Data for VVD-214

M. Wt 437.46
Formula C20H21F2N3O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 3026500-20-6
PubChem ID 38658751
InChI Key UWPFUBNCDABUEE-SIFUEBAJSA-N
Smiles CS(/C=C/[C@H](C1CC1)NC(C(C(OC2=CC=CC=C2)=N3)=CN=C3C(F)(F)C)=O)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for VVD-214

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.87 50

Preparing Stock Solutions for VVD-214

The following data is based on the product molecular weight 437.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.57 mL 22.86 mL 45.72 mL
2.5 mM 0.91 mL 4.57 mL 9.14 mL
5 mM 0.46 mL 2.29 mL 4.57 mL
25 mM 0.09 mL 0.46 mL 0.91 mL

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References for VVD-214

References are publications that support the biological activity of the product.

Kikuchi et al (2025) Identification of VVD-214/RO7589831, a clinical-stage, covalent allosteric inhibitor of WRN helicase for the treatment of MSI-high cancers. J.Med.Chem. 68 25912 PMID: 40964743

Baltgalvis et al (2024) Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase. Nature 629 435 PMID: 38658751

If you know of a relevant reference for VVD-214, please let us know.

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Citations for VVD-214

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