PROTAC IRAK4 degrader-1

Name: PROTAC IRAK4 degrader-1
Brand: MedChemExpress
SKU: HY-129966
Rating: 4.5 (1 reviews)

Cat. No.: HY-129966 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.

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

PROTAC IRAK4 degrader-1 Chemical Structure

CAS No. : 2360533-90-8

Size	Price	Stock	Quantity
1 mg	USD 568	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1950	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3850	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 6200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 9200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PROTAC IRAK4 degrader-1

•Blood. 2023 May 12;blood.2022018718. [Abstract]

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IRAK1 IRAK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IRAK4

Cereblon

Molecular Weight

904.85

Formula

C₄₄H₃₉F₃N₁₂O₇

CAS No.

2360533-90-8

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC=C(N2C=C(NC(C3=COC(C4=CC=NC(NCC5CC5)=C4)=N3)=O)C(C(F)(F)F)=N2)C=C1)NCCCN(C=N6)C=C6CNC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8=O)=O)=CC=C7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL (121.57 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	1.1052 mL	5.5258 mL	11.0516 mL
5 mM	0.2210 mL	1.1052 mL	2.2103 mL
10 mM	0.1105 mL	0.5526 mL	1.1052 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 (sealed storage, away from moisture). 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: ≥ 5.25 mg/mL (5.80 mM); Clear solution

This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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 (5.53 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 (sealed storage, away from moisture)

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: 99.72%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (254 KB) HNMR (382 KB) LCMS (129 KB)

Handling Instructions (2659 KB)

References

[1]. Nello Mainolfi, et al. Irak degraders and uses thereof. US20190192668A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.1052 mL	5.5258 mL	11.0516 mL	27.6289 mL
	5 mM	0.2210 mL	1.1052 mL	2.2103 mL	5.5258 mL
	10 mM	0.1105 mL	0.5526 mL	1.1052 mL	2.7629 mL
	15 mM	0.0737 mL	0.3684 mL	0.7368 mL	1.8419 mL
	20 mM	0.0553 mL	0.2763 mL	0.5526 mL	1.3814 mL
	25 mM	0.0442 mL	0.2210 mL	0.4421 mL	1.1052 mL
	30 mM	0.0368 mL	0.1842 mL	0.3684 mL	0.9210 mL
	40 mM	0.0276 mL	0.1381 mL	0.2763 mL	0.6907 mL
	50 mM	0.0221 mL	0.1105 mL	0.2210 mL	0.5526 mL
	60 mM	0.0184 mL	0.0921 mL	0.1842 mL	0.4605 mL
	80 mM	0.0138 mL	0.0691 mL	0.1381 mL	0.3454 mL
	100 mM	0.0111 mL	0.0553 mL	0.1105 mL	0.2763 mL