VVD 065

Product Description

VVD 065 is a NRF2 inhibitor acting via a covalent allosteric molecular glue mechanism. Through covalent engagement of C151 on KEAP1, VVD 065 promotes NRF2 degradation by enhancing formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target engagement (TE₅₀ = 9 nm in KYSE70 cells) and selectivity over unrelated targets, VVD 065 inhibits NRF2-dependent cell growth. In vitro, VVD 065 inhibits NRF2 transcriptional activity and reduces the expression of NRF2 target genes. In vivo, VVD 065 induces tumor growth inhibition and downregulation of NRF2 signaling in cell-line and patient-derived mouse xenograft models, synergizing with other combinations. VVD 065 is orally bioavailable.

Licensing Information

Sold with permission from Vividion Therapeutics.

Solubility

Preparing Stock Solutions for VVD 065

The following data is based on the product molecular weight 345.79

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.89 mL	14.46 mL	28.92 mL
5 mM	0.58 mL	2.89 mL	5.78 mL
10 mM	0.29 mL	1.45 mL	2.89 mL
50 mM	0.06 mL	0.29 mL	0.58 mL

Calculators