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VVD 065

Cat. No. 8875 Submit a Review Datasheet / COA / SDS
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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)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data for VVD 065

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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References for VVD 065

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

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Citations for VVD 065

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

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