Homo-PROTAC pVHL30 degrader 1

Name: Homo-PROTAC pVHL30 degrader 1
Brand: MedChemExpress
SKU: HY-111593
Rating: 4.5 (1 reviews)

Cat. No.: HY-111593 Purity: 99.40%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.

For research use only. We do not sell to patients.

Homo-PROTAC pVHL30 degrader 1 Chemical Structure

CAS No. : 2244684-49-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1020	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Homo-PROTAC pVHL30 degrader 1

•Structure. 2024 Sep 28:S0969-2126(24)00385-X. [Abstract]

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC^[1], consists of two ligands of von Hippel-Lindau.

IC₅₀ & Target

VHL

In Vitro

Homo-PROTAC pVHL30 degrader 1 dimerizes von Hippel-Lindau (VHL) with high avidity in vitro and induces potent, rapid and proteasome-dependent self-degradation of VHL in different cell lines, in a highly isoform-selective fashion and without triggering a hypoxic response^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1179.45

Formula

C₅₈H₈₂N₈O₁₄S₂

CAS No.

2244684-49-7

Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C2=CC=C(CNC([C@@H]3C[C@@]([H])(O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@]([H])(O)C4)=O)=O)=O)=O)=O)C=C2)SC=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : ≥ 150 mg/mL (127.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (21.20 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.8479 mL	4.2393 mL	8.4785 mL
5 mM	0.1696 mL	0.8479 mL	1.6957 mL
10 mM	0.0848 mL	0.4239 mL	0.8479 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 (stored under nitrogen). 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.40%

Select Batch:

Data Sheet (268 KB) SDS (393 KB)

COA (242 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Maniaci C, et al. Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nat Commun. 2017 Oct 10;8(1):830. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	0.8479 mL	4.2393 mL	8.4785 mL	21.1963 mL
	5 mM	0.1696 mL	0.8479 mL	1.6957 mL	4.2393 mL
	10 mM	0.0848 mL	0.4239 mL	0.8479 mL	2.1196 mL
	15 mM	0.0565 mL	0.2826 mL	0.5652 mL	1.4131 mL
	20 mM	0.0424 mL	0.2120 mL	0.4239 mL	1.0598 mL
DMSO	25 mM	0.0339 mL	0.1696 mL	0.3391 mL	0.8479 mL
	30 mM	0.0283 mL	0.1413 mL	0.2826 mL	0.7065 mL
	40 mM	0.0212 mL	0.1060 mL	0.2120 mL	0.5299 mL
	50 mM	0.0170 mL	0.0848 mL	0.1696 mL	0.4239 mL
	60 mM	0.0141 mL	0.0707 mL	0.1413 mL	0.3533 mL
	80 mM	0.0106 mL	0.0530 mL	0.1060 mL	0.2650 mL
	100 mM	0.0085 mL	0.0424 mL	0.0848 mL	0.2120 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.