VVD-214

VVD-214
Clinical data
Drug class	WRN helicase inhibitor
Identifiers
	IUPAC name N-[(E,1S)-1-cyclopropyl-3-methylsulfonylprop-2-enyl]-2-(1,1-difluoroethyl)-4-phenoxypyrimidine-5-carboxamide;
CAS Number	3026500-20-6;
PubChem CID	170717998;
ChemSpider	129389587;
Chemical and physical data
Formula	C20H21F2N3O4S
Molar mass	437.46 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C1=NC=C(C(=N1)OC2=CC=CC=C2)C(=O)N[C@H](/C=C/S(=O)(=O)C)C3CC3)(F)F;
	InChI InChI=1S/C20H21F2N3O4S/c1-20(21,22)19-23-12-15(18(25-19)29-14-6-4-3-5-7-14)17(26)24-16(13-8-9-13)10-11-30(2,27)28/h3-7,10-13,16H,8-9H2,1-2H3,(H,24,26)/b11-10+/t16-/m1/s1; Key:UWPFUBNCDABUEE-SIFUEBAJSA-N;

VVD-214 (RO7589831) is a drug which acts as an inhibitor of the enzyme WRN helicase. It is being researched for the treatment of microsatellite instability high forms of cancer.^[1]^[2]

References

^ Kikuchi S, Green JC, Rogness DC, Lam B, Owyang ZA, Malmstrom RD, et al. (December 2025). "Identification of VVD-214/RO7589831, a Clinical-Stage, Covalent Allosteric Inhibitor of WRN Helicase for the Treatment of MSI-High Cancers". Journal of Medicinal Chemistry. 68 (24): 25912–25938. doi:10.1021/acs.jmedchem.5c01805. PMC 12751020. PMID 40964743.
^ Baltgalvis KA, Lamb KN, Symons KT, Wu CC, Hoffman MA, Snead AN, et al. (May 2024). "Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase". Nature. 629 (8011): 435–442. doi:10.1038/s41586-024-07318-y. PMID 38658751.

[1] Kikuchi S, Green JC, Rogness DC, Lam B, Owyang ZA, Malmstrom RD, et al. (December 2025). "Identification of VVD-214/RO7589831, a Clinical-Stage, Covalent Allosteric Inhibitor of WRN Helicase for the Treatment of MSI-High Cancers". Journal of Medicinal Chemistry. 68 (24): 25912–25938. doi:10.1021/acs.jmedchem.5c01805. PMC 12751020. PMID 40964743.

[2] Baltgalvis KA, Lamb KN, Symons KT, Wu CC, Hoffman MA, Snead AN, et al. (May 2024). "Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase". Nature. 629 (8011): 435–442. doi:10.1038/s41586-024-07318-y. PMID 38658751.

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