Chemical Structure : VVD-065
CAS No.:
3034876-85-9
VVD-065
(VVD065)
Catalog No.: PC-25485Not For Human Use, Lab Use Only.
VVD-065 is a first-in-class, allosteric molecular glue of Keap1-Cul3 E3-ligase complex and NRF2 inhibitor, specifically and covalently engages C151 on KEAP1 with engagement potency (TE50) of 9 nM in KYSE70 cells, promotes KEAP1-CUL3 complex formation, leading to enhancement of NRF2 degradation.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
VVD-065 is a first-in-class, allosteric molecular glue of Keap1-Cul3 E3-ligase complex and NRF2 inhibitor, specifically and covalently engages C151 on KEAP1 with engagement potency (TE50) of 9 nM in KYSE70 cells, promotes KEAP1-CUL3 complex formation, leading to enhancement of NRF2 degradation.
VVD-065 covalently binds C151 of KEAP1, may increase KEAP1 activity by stabilizing a KEAP1 conformation that favors CUL3 binding.
VVD-065 induces robust degradation of NRF2 and decreases expression of NRF2 target genes.
VVD-065 (5-25 mg/kg) exhibits cancer cell growth inhibitory effects. VVD-065 exhibits anti-tumorigenic effects in KYSE70 tumor bearing animals
VVD-065 exhibits strong antitumor effects in syngeneic with cisplatin and nab-paclitaxel in various solid tumor types such as NSCLC, ESCC, HNSCC, and uterine cancers.
Physicochemical Properties
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M.Wt
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345.79
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Formula
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C16H16ClN5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-1-(3-(3-(4-amino-1,3,5-triazin-2-yl)-5-chlorophenyl)morpholino)prop-2-en-1-one
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References
1. Nilotpal Roy, et al. Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glue. bioRxiv, 2024, preprint, 10.1101/2024.10.04.616592.
2. Nil Roy, et al. Mol Cancer Ther (2023) 22 (12_Supplement): PR011.
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