Art. -Nr.: HY-16684

AGN-195183

(Synonyms: IRX-5183; VTP-195183; NRX-195183)

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Based on 1 Customer Validation

AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (K_d=3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.

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Reinheit: 99.75%
CAS. Nr.: 367273-07-2
Formel: C₂₂H₂₂ClF₂NO₄
Molecular Weight:437.86

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AGN-195183 Chemical Structure

CAS. Nr.: 367273-07-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (K_d=3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.

IC₅₀ & Target

IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans)

Alle RAR/RXR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-BR-3	IC₅₀	11 nM Compound: 4 (AGN-195183)	Inhibition of ER-negative human breast cancer cell SK-BR-3 proliferation Inhibition of ER-negative human breast cancer cell SK-BR-3 proliferation	[PMID: 12372520]
T47D	IC₅₀	1.4 nM Compound: 4 (AGN-195183)	Inhibition of ER positive human breast cancer cell T-47D proliferation Inhibition of ER positive human breast cancer cell T-47D proliferation	[PMID: 12372520]

In Vitro

AGN-195183 (IRX-5183; Compound 4) inhibits the growth of breast cancer cell lines, and is inactive in an in vivo model of topical irritation. AGN-195183 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3. AGN-195183 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. AGN-195183 is currently in Phase I/IIA clinical trials in cancer patients.

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 367273-07-2
Appearance Solid
Molecular Weight 437.86
Formel C₂₂H₂₂ClF₂NO₄
Color White to off-white
SMILES

O=C(O)C1=C(F)C=C(NC(C2=C(O)C(Cl)=C3C(C)(C)CCC(C)(C)C3=C2)=O)C=C1F
Synonyms

IRX-5183; VTP-195183; NRX-195183
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 11 mg/mL (25.12 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

2.2838 mL

11.4192 mL

22.8384 mL

5 mM

0.4568 mL

2.2838 mL

4.5677 mL

10 mM

0.2284 mL

1.1419 mL

2.2838 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.1 mg/mL (2.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.1 mg/mL (2.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.1 mg/mL (2.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 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 (11.0 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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2838 mL	11.4192 mL	22.8384 mL	57.0959 mL
	5 mM	0.4568 mL	2.2838 mL	4.5677 mL	11.4192 mL
	10 mM	0.2284 mL	1.1419 mL	2.2838 mL	5.7096 mL
	15 mM	0.1523 mL	0.7613 mL	1.5226 mL	3.8064 mL
	20 mM	0.1142 mL	0.5710 mL	1.1419 mL	2.8548 mL
	25 mM	0.0914 mL	0.4568 mL	0.9135 mL	2.2838 mL

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AGN-195183

Differentiation Inducing Compound Library

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Anti-Breast Cancer Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AGN-195183

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Transcription Factor-Targeted Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AGN-195183 Related Classifications

HY-16684 Related Classifications