Art. -Nr.: HY-151886

NU223612

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NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a K_d of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB).

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Reinheit: 99.41%
CAS. Nr.: 2759420-43-2
Formel: C₄₉H₅₅FN₆O₉
Molecular Weight:890.99

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NU223612 Chemical Structure

CAS. Nr.: 2759420-43-2

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Preis

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Cereblon

IDO1

640 nM (Kd)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen :

In Vitro

NU223612 (0.1-10 μM; 24 h) decreases IDO1 protein levels dose-dependently^[1].
A DC₅₀ (the concentration of the NU223612 at which 50% of the IDO1 protein is degraded) of 0.3290 μM and 0.5438 μM in U87 and GBM43 cells is determined, respectively^[1].
NU223612 degrades IDO1 protein in multiple cell types, such as CD18 and PANC-1 human pancreatic cancer cells, OVCAR5 and SKOV3 human ovarian cancer cells, PC3 human prostate cancer cells, and the syngeneic GL261 mouse IDO1 cDNA-expressing (IDO1-O/E) glioma cell line^[1].
NU223612 equally degrades IDO1 protein levels in both the cytoplasmic and nuclear intracellular compartments in human GBM cells. NU223612 is able to penetrate subcellular compartments^[1].
NU223612 dose-dependently inhibits IDO1 enzyme activity resulting in decreased Kyn levels in cultured IFNγ-stimulated GBM cells. NU223612 inhibits both IDO1-mediated tryptophan metabolism as well as IDO1 non-enzyme-mediated NF-κB p65 transcription factor DNA binding activity^[1].

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

Western Blot Analysis^[1]

Cell Line:

U87 and human GBM43 cells
Concentration:

0 μM, 0.1 μM, 1 μM, and 10 μM
Incubation Time:

24 h
Result:

Decreased IDO1 protein levels dose-dependently.

In Vivo

NU223612 (25 mg/kg; i.p.; once) decreases IDO1 protein in C57BL/6 with mIDO1 cDNA-expressing GL261 cells^[1].
NU223612 (25 mg/kg; i.p.; 5 days/week; for 3 weeks) leads to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection^[1].
Mass spectrometry analysis of NU223612 (25 mg/kg; i.p.; once) shows a C_max of 2 μM and a half-life of 8.3 h in brain tissue. In plasma, C_max is 365 μM and the half-life is 2.5 h. The binding of NU223612 to mouse brain homogenate using a 6 h equilibrium dialysis shows NU223612 to be 99.8% bound^[1].
Half-life, AUC, and C_max of NU223612 in serum and brain samples^[1].

	Plasma	Brain
half-lifr (h)	2.5	8.3
AUC_0-24 (μM h)	582	7
C_max (μM)	365	2

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

Animal Model:

Male C57BL/6 mice bearing GL261 cells^[1]
Dosage:

25 mg/kg
Administration:

i.p.; once
Result:

Decreased IDO1 protein by >70% within 2 h post-treatment and remains low for up to 24 h.

Animal Model:

8 week old C57BL/6 wild-type (WT) mice are intracranially engrafted with luciferase-modified GL261 cells (GL261-luc.)^[1]
Dosage:

25 mg/kg
Administration:

i.p.; 5 days/week; for 3 weeks
Result:

Led to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection.

Chemical Information

CAS. Nr. 2759420-43-2
Appearance Solid
Molecular Weight 890.99
Formel C₄₉H₅₅FN₆O₉
Color White to yellow
SMILES

O=C([C@H](C)[C@@]1([H])CC[C@](C2=CC=NC3=CC=C(F)C=C23)([H])CC1)NC4=CC=C(OC5CCN(C(CCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)CC5)C=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (112.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1223 mL

5.6117 mL

11.2235 mL

5 mM

0.2245 mL

1.1223 mL

2.2447 mL

10 mM

0.1122 mL

0.5612 mL

1.1223 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lakshmi R Bollu, et al. Identification and Characterization of a Novel Indoleamine 2,3-Dioxygenase 1 Protein Degrader for Glioblastoma. J Med Chem. 2022 Nov 21. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1223 mL	5.6117 mL	11.2235 mL	28.0587 mL
	5 mM	0.2245 mL	1.1223 mL	2.2447 mL	5.6117 mL
	10 mM	0.1122 mL	0.5612 mL	1.1223 mL	2.8059 mL
	15 mM	0.0748 mL	0.3741 mL	0.7482 mL	1.8706 mL
	20 mM	0.0561 mL	0.2806 mL	0.5612 mL	1.4029 mL
	25 mM	0.0449 mL	0.2245 mL	0.4489 mL	1.1223 mL
	30 mM	0.0374 mL	0.1871 mL	0.3741 mL	0.9353 mL
	40 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7015 mL
	50 mM	0.0224 mL	0.1122 mL	0.2245 mL	0.5612 mL
	60 mM	0.0187 mL	0.0935 mL	0.1871 mL	0.4676 mL
	80 mM	0.0140 mL	0.0701 mL	0.1403 mL	0.3507 mL
	100 mM	0.0112 mL	0.0561 mL	0.1122 mL	0.2806 mL

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NU223612

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Pancreatic Cancer Compound Library

Metabolic Enzyme Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NU223612

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Pancreatic Cancer Compound Library

Metabolic Enzyme Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NU223612 Related Classifications

HY-151886 Related Classifications