2. PROTAC
  3. Ligands for E3 Ligase
  4. VHL Ligand 8

VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.

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VHL Ligand 8 Chemical Structure

VHL Ligand 8 Chemical Structure

CAS No. : 2701565-76-4

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Based on 1 publication(s) in Google Scholar

VHL Ligand 8 Related Antibodies

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP

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Description

VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM[1].

IC50 & Target[1]

VHL

 

Molecular Weight

443.49

Formula

C23H29N3O6
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

OC(C[C@@H](C1=CC=CC=C1)NC([C@H]2N(C([C@H](C(C)C)C3=CC(C)=NO3)=O)C[C@H](O)C2)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (225.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (56.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2548 mL 11.2742 mL 22.5484 mL
5 mM 0.4510 mL 2.2548 mL 4.5097 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (112.74 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.2548 mL 11.2742 mL 22.5484 mL 56.3711 mL
5 mM 0.4510 mL 2.2548 mL 4.5097 mL 11.2742 mL
10 mM 0.2255 mL 1.1274 mL 2.2548 mL 5.6371 mL
15 mM 0.1503 mL 0.7516 mL 1.5032 mL 3.7581 mL
20 mM 0.1127 mL 0.5637 mL 1.1274 mL 2.8186 mL
25 mM 0.0902 mL 0.4510 mL 0.9019 mL 2.2548 mL
30 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8790 mL
40 mM 0.0564 mL 0.2819 mL 0.5637 mL 1.4093 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1274 mL
DMSO 60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9395 mL
80 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7046 mL
100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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VHL Ligand 8 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VHL Ligand 82701565-76-4VHL Ligand8VHL Ligand-8Ligands for E3 LigaseE3 ligase-recruiting MoietyVHLligandARD-266androgenreceptorInhibitorinhibitorinhibit

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