PROTAC RAR Degrader-1

Name: PROTAC RAR Degrader-1
Brand: MedChemExpress
SKU: HY-111844
Rating: 4.5 (1 reviews)

Cat. No.: HY-111844 Purity: 97.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)).

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

PROTAC RAR Degrader-1 Chemical Structure

CAS No. : 1351169-27-1

Size	Price	Stock	Quantity
1 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 950	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

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View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All RAR/RXR Isoform Specific Products:

View All Isoforms

RXRα RXRβ RXRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

cIAP1

RXR α

In Vitro

PROTAC RAR degrader-1 (1-30 μM; 24 h) reduces RAR level in a concentration dependent manner and has no effect on CRABP-II in HT1080 cells expressing flag-labeled cIAP1^[1].

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

Western Blot Analysis^[1]

Cell Line:	HT1080 cells expressing Flag-tagged cIAP1
Concentration:	1, 10 and 30 μM
Incubation Time:	24 h
Result:	Significantly reduced the level of RARα, but CRABP-II did not change.

Molecular Weight

917.14

Formula

C₅₁H₇₂N₄O₁₁

CAS No.

1351169-27-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(/C=C/C(C2=CC(C(C)(C)C)=CC(C(C)(C)C)=C2)=O)C=C1OCCCNC(COCCOCCOCCNC([C@H](CC(C)C)NC([C@@H](O)[C@H](N)CC3=CC=CC=C3)=O)=O)=O

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 : ≥ 80 mg/mL (87.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0903 mL	5.4517 mL	10.9035 mL
5 mM	0.2181 mL	1.0903 mL	2.1807 mL
10 mM	0.1090 mL	0.5452 mL	1.0903 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

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 mg/mL (2.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (2.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (2.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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.

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

Purity: 97.91%

Select Batch:

Data Sheet (269 KB) SDS (252 KB)

COA (242 KB) HNMR (313 KB) RP-HPLC (245 KB) MS (69 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]

[2]. Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.0903 mL	5.4517 mL	10.9035 mL	27.2587 mL
	5 mM	0.2181 mL	1.0903 mL	2.1807 mL	5.4517 mL
	10 mM	0.1090 mL	0.5452 mL	1.0903 mL	2.7259 mL
	15 mM	0.0727 mL	0.3634 mL	0.7269 mL	1.8172 mL
	20 mM	0.0545 mL	0.2726 mL	0.5452 mL	1.3629 mL
	25 mM	0.0436 mL	0.2181 mL	0.4361 mL	1.0903 mL
	30 mM	0.0363 mL	0.1817 mL	0.3634 mL	0.9086 mL
	40 mM	0.0273 mL	0.1363 mL	0.2726 mL	0.6815 mL
	50 mM	0.0218 mL	0.1090 mL	0.2181 mL	0.5452 mL
	60 mM	0.0182 mL	0.0909 mL	0.1817 mL	0.4543 mL
	80 mM	0.0136 mL	0.0681 mL	0.1363 mL	0.3407 mL