VVD 065 |
カタログ番号GC81040
One-Click Copy Product Info
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VVD 065 is an orally active KEAP1 -dependent NRF2 molecular glue degrader with a KEAP1 K D of 65 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3034876-85-9
Sample solution is provided at 25 µL, 10mM.
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In Vivo, VVD-065 (0.3-50 mg/kg; p.o.; QD or BID) induces robust NRF2 degradation and tumor growth inhibition in KYSE70 xenograft mice[3]. VVD-065 (2-50 mg/kg; p.o.; QD or BID) produces potent, sustained tumor growth inhibition in HCC95 xenograft mice[3]. VVD-065 (50 mg/kg; p.o.; QD or BID) drives tumor growth inhibition in diverse PDX models[3]. VVD-065 (50 mg/kg; p.o.; QD) improves overall survival and reduces tumor burden in orthotopic KLN-205 syngeneic mice[3].
In Vitro, VVD 065 potently reduces NRF2 protein levels in wild-type KEAP1/NRF2, KEAP1-mutant, and NRF2-mutant cellular settings, inhibits NRF2-dependent gene expression, and suppresses proliferation of NRF2-dependent cancer cell lines at low nM concentrations[2].
References:
[1]. Adamopoulos C, et al. Turning KEAP1 against NRF2. Nat Chem Biol. 2026 May;22(5):680-682.
[2]. Roy N, et al. Abstract PR011: Discovery of VVD-065, a first-in class allosteric molecular glue of the Keap1-Cul3 E3-ligase complex for the treatment of NRF2 activated cancers. Mol Cncer Ther. 2023 Dec 01;22:PR011.
[3]. Roy N, et al. A Covalent Allosteric Molecular Glue Suppresses NRF2-Dependent Cancer Growth. Cancer Discov. 2026 May 1;16(5):953-975.
| Cas No. | 3034876-85-9 | SDF | |
| Formula | C16H16ClN5O2 | M.Wt | 345.78 |
| 溶解度 | Storage | Store at 4°C, stored under nitrogen | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.892 mL | 14.4601 mL | 28.9201 mL |
| 5 mM | 578.4 μL | 2.892 mL | 5.784 mL |
| 10 mM | 289.2 μL | 1.446 mL | 2.892 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)