PROTAC AR Degrader-4

Cat. No.: HY-111848: FAQs
Data Sheet Handling Instructions

Molarity Calculator

PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PROTAC AR Degrader-4 TFA) usually boasts enhanced water solubility and stability.

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

PROTAC AR Degrader-4 Chemical Structure

CAS No. : 1351169-31-7

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Other Forms of PROTAC AR Degrader-4:

PROTAC AR Degrader-4 TFA Get quote

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

cIAP1

In Vitro

Specific and Nongenetic IAPs-dependent Protein Erasers (SNIPERs) are bifunctional compounds which are designed by conjugating an IAPs-recognition structure with a target protein-recognition structure.
Targeting proteins for degradation involves three steps.
1, its two recognition structures allow SNIPER to form a complex linking IAPs, which have E3 ligase activity, with the target protein.
2, the target protein is polyubiquitinated by IAPs.
3, the polyubiquitinated protein is degraded by proteasome.

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

Molecular Weight

770.01

Formula

C₄₃H₆₇N₃O₉

CAS No.

1351169-31-7

SMILES

O=C1CC[C@@]2(C)[C@](CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@@H]4OC(COCCOCCOCCNC([C@H](CC(C)C)NC([C@@H](O)[C@H](N)CC5=CC=CC=C5)=O)=O)=O)([H])C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (259.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.2987 mL	6.4934 mL	12.9868 mL
5 mM	0.2597 mL	1.2987 mL	2.5974 mL
10 mM	0.1299 mL	0.6493 mL	1.2987 mL

View the Complete Stock Solution Preparation Table

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: ≥ 5 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 5 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.2987 mL	6.4934 mL	12.9868 mL	32.4671 mL
	5 mM	0.2597 mL	1.2987 mL	2.5974 mL	6.4934 mL
	10 mM	0.1299 mL	0.6493 mL	1.2987 mL	3.2467 mL
	15 mM	0.0866 mL	0.4329 mL	0.8658 mL	2.1645 mL
	20 mM	0.0649 mL	0.3247 mL	0.6493 mL	1.6234 mL
	25 mM	0.0519 mL	0.2597 mL	0.5195 mL	1.2987 mL
	30 mM	0.0433 mL	0.2164 mL	0.4329 mL	1.0822 mL
	40 mM	0.0325 mL	0.1623 mL	0.3247 mL	0.8117 mL
	50 mM	0.0260 mL	0.1299 mL	0.2597 mL	0.6493 mL
	60 mM	0.0216 mL	0.1082 mL	0.2164 mL	0.5411 mL
	80 mM	0.0162 mL	0.0812 mL	0.1623 mL	0.4058 mL
	100 mM	0.0130 mL	0.0649 mL	0.1299 mL	0.3247 mL