VVD-214, also known as RO7589831 and VVD 133214, is an oral covalent, reversible, and allosteric inhibitor of WRN helicase. VD-133214 selectively engages a cysteine (C727) located in a region of the helicase domain subject to interdomain movement during DNA unwinding. VVD-133214 binds WRN protein cooperatively with nucleotide and stabilizes compact conformations lacking the dynamic flexibility necessary for proper helicase function, resulting in widespread double-stranded DNA breaks, nuclear swelling and cell death in MSI-high (MSI-H), but not in microsatellite-stable, cells. VVD-214 was well tolerated in mice and led to robust tumour regression in multiple MSI-H colorectal cancer cell lines and patient-derived xenograft models.
MedKoo Cat#: 126857
Name: VVD-214
CAS#: 3026500-20-6
Chemical Formula: C20H21F2N3O4S
Exact Mass: 437.1221
Molecular Weight: 437.46
Elemental Analysis: C, 54.91; H, 4.84; F, 8.69; N, 9.61; O, 14.63; S, 7.33
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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
