| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
VHL
VL285 targets the von Hippel-Lindau (VHL) E3 ubiquitin ligase. By incorporating VL285, a PROTAC can effectively "hijack" the VHL E3 ligase to degrade a target protein of interest. It binds to VHL with high affinity and is used in the synthesis of PROTAC molecules. |
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| ln Vitro |
The ability of HaloPROTAC3 to cause GFP-HaloTag7 degradation is lessened when VL285 is treated[1].
In vitro, the activity of VL285 is assessed as part of the final PROTAC molecule. The effectiveness of a PROTAC incorporating VL285 is measured by its ability to degrade the target protein. |
| ln Vivo |
In vivo, the efficacy of VL285 is evaluated as part of a complete PROTAC molecule in animal models to assess target protein degradation and downstream pharmacological effects.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for VL285 involve measuring its binding affinity to the VHL protein. This is typically done using surface plasmon resonance (SPR). The Kd for VHL binding is determined.
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| Cell Assay |
In vitro cell-based experiments for VL285 are performed using cells expressing the target protein of interest. The cells are treated with a PROTAC molecule that incorporates VL285. Target protein levels are measured by Western blot to assess degradation.
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| Animal Protocol |
In vivo animal experiments for VL285 are conducted using xenograft or other animal models. A complete PROTAC molecule containing VL285 is administered, and target protein degradation and pharmacological effects are assessed.
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| ADME/Pharmacokinetics |
VL285 is a chemical building block used in PROTAC synthesis. Its properties are defined by its chemical structure.
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| Toxicity/Toxicokinetics |
VL285 is a chemical reagent used in research. Its toxicity is assessed as part of the final PROTAC molecule.
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| References | |
| Additional Infomation |
VL285 is also known as (S,R,S)-VL285 Phenol. It is a research tool for PROTAC technology and is not a therapeutic agent itself.
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| Molecular Formula |
C29H32N4O4S
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|---|---|
| Molecular Weight |
532.653785705566
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| Exact Mass |
532.214
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| Elemental Analysis |
C, 65.39; H, 6.06; N, 10.52; O, 12.01; S, 6.02
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| CAS # |
1448188-57-5
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| Related CAS # |
1448188-57-5
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| PubChem CID |
71667162
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
879
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)C)N4CC5=CC=CC=C5C4=O)O
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| InChi Key |
HEDFFPYRFJKXQP-VJTSUQJLSA-N
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| InChi Code |
InChI=1S/C29H32N4O4S/c1-17(2)25(33-14-21-6-4-5-7-23(21)28(33)36)29(37)32-15-22(34)12-24(32)27(35)30-13-19-8-10-20(11-9-19)26-18(3)31-16-38-26/h4-11,16-17,22,24-25,34H,12-15H2,1-3H3,(H,30,35)/t22-,24+,25+/m1/s1
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| Chemical Name |
(2S,4R)-4-Hydroxy-1-((S)-3-methyl-2-(1-oxoisoindolin-2-yl)butanoyl)-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
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| Synonyms |
VL-285; VL 285; VL285
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL ( 187.74 mM )
Ethanol : 50 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8774 mL | 9.3870 mL | 18.7741 mL | |
| 5 mM | 0.3755 mL | 1.8774 mL | 3.7548 mL | |
| 10 mM | 0.1877 mL | 0.9387 mL | 1.8774 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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