PROTAC AR Degrader-4 TFA

Name: PROTAC AR Degrader-4 TFA
Brand: MedChemExpress
SKU: HY-111848A
Rating: 4.5 (1 reviews)

Cat. No.: HY-111848A: FAQs
Data Sheet SDS 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).

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

PROTAC AR Degrader-4 TFA Chemical Structure

Size	Price	Stock	Quantity
1 mg	USD 630	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PROTAC AR Degrader-4 TFA:

PROTAC AR Degrader-4 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

884.03

Formula

C₄₅H₆₈F₃N₃O₁₁

Appearance

Solid

Color

White to off-white

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.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (113.12 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	1.1312 mL	5.6559 mL	11.3118 mL
5 mM	0.2262 mL	1.1312 mL	2.2624 mL
10 mM	0.1131 mL	0.5656 mL	1.1312 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.

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

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 (5.66 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 (5.66 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).

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

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

Data Sheet (271 KB) SDS (251 KB) 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	1.1312 mL	5.6559 mL	11.3118 mL	28.2796 mL
	5 mM	0.2262 mL	1.1312 mL	2.2624 mL	5.6559 mL
	10 mM	0.1131 mL	0.5656 mL	1.1312 mL	2.8280 mL
	15 mM	0.0754 mL	0.3771 mL	0.7541 mL	1.8853 mL
	20 mM	0.0566 mL	0.2828 mL	0.5656 mL	1.4140 mL
	25 mM	0.0452 mL	0.2262 mL	0.4525 mL	1.1312 mL
	30 mM	0.0377 mL	0.1885 mL	0.3771 mL	0.9427 mL
	40 mM	0.0283 mL	0.1414 mL	0.2828 mL	0.7070 mL
	50 mM	0.0226 mL	0.1131 mL	0.2262 mL	0.5656 mL
	60 mM	0.0189 mL	0.0943 mL	0.1885 mL	0.4713 mL
	80 mM	0.0141 mL	0.0707 mL	0.1414 mL	0.3535 mL
	100 mM	0.0113 mL	0.0566 mL	0.1131 mL	0.2828 mL