VVD 065

Name: VVD 065
Brand: Tocris Bioscience
SKU: 8875

Tocris Bioscience, part of Bio-Techne | Catalog # 8875

COA / SDS

Covalent allosteric NRF2 inhibitor

Key Product Details

Description:	Covalent allosteric NRF2 inhibitor
Chemical Name:	1-[(3R)-3-[3-(4-Amino-1,3,5-triazin-2-yl)-5-chlorophenyl]-4-morpholinyl]-2-propen-1-one
Purity:	≥98% (HPLC)
Molecular Weight:	345.79

View Full Technical Details for VVD 065

Technical Data
Citations

Biological Activity for VVD 065

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.

Technical Data for VVD 065

M. Wt	345.79
Formula	C₁₆H₁₆ClN₅O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	3034876-85-9
PubChem ID	171499181
InChi Key	BMXYLROANWRSJZ-ZDUSSCGKSA-N
Smiles	C=CC(N1[C@H](C2=CC(C3=NC=NC(N)=N3)=CC(Cl)=C2)COCC1)=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 for VVD 065

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	34.58	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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Product Documents for VVD 065

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.