PROTAC IDO1 Degrader-1

Name: PROTAC IDO1 Degrader-1
Brand: MedChemExpress
SKU: HY-131911
Rating: 4.5 (1 reviews)

Cat. No.: HY-131911 Purity: 98.17%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC₅₀=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells.

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

PROTAC IDO1 Degrader-1 Chemical Structure

CAS No. : 2488851-89-2

Size	Price	Stock	Quantity
5 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 4500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 7200	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

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

IDO1

2.84 μM (DC₅₀)

IDO1

1.07 μM (IC₅₀)

In Vitro

PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ^[1].
PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells^[1].
PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	HeLa cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Notably decreased IDO1 level induced by IFN-γ (5 ng/mL).

Molecular Weight

966.80

Formula

C₄₀H₅₃BrFN₉O₁₃

CAS No.

2488851-89-2

Appearance

Solid

Color

Yellow to brown

SMILES

O=C1C2=C(NCCOCCOCCOCCOCCOCCOCCOCCNCCNC3=NON=C3/C(NC4=CC(Br)=C(C=C4)F)=N/O)C=CC=C2C(N1C5C(NC(CC5)=O)=O)=O

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 : 100 mg/mL (103.43 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	1.0343 mL	5.1717 mL	10.3434 mL
5 mM	0.2069 mL	1.0343 mL	2.0687 mL
10 mM	0.1034 mL	0.5172 mL	1.0343 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

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 (5.17 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 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 (5.17 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: 98.17%

Select Batch:

Data Sheet (270 KB) SDS (251 KB)

COA (244 KB) HNMR (224 KB) LCMS (129 KB)

Handling Instructions (2659 KB)

References

[1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.0343 mL	5.1717 mL	10.3434 mL	25.8585 mL
	5 mM	0.2069 mL	1.0343 mL	2.0687 mL	5.1717 mL
	10 mM	0.1034 mL	0.5172 mL	1.0343 mL	2.5859 mL
	15 mM	0.0690 mL	0.3448 mL	0.6896 mL	1.7239 mL
	20 mM	0.0517 mL	0.2586 mL	0.5172 mL	1.2929 mL
	25 mM	0.0414 mL	0.2069 mL	0.4137 mL	1.0343 mL
	30 mM	0.0345 mL	0.1724 mL	0.3448 mL	0.8620 mL
	40 mM	0.0259 mL	0.1293 mL	0.2586 mL	0.6465 mL
	50 mM	0.0207 mL	0.1034 mL	0.2069 mL	0.5172 mL
	60 mM	0.0172 mL	0.0862 mL	0.1724 mL	0.4310 mL
	80 mM	0.0129 mL	0.0646 mL	0.1293 mL	0.3232 mL
	100 mM	0.0103 mL	0.0517 mL	0.1034 mL	0.2586 mL