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Art. -Nr.: HY-149085

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XS-060

Kundenbewertung

Based on 1 Customer Validation

XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome.

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Reinheit: 98.67%
CAS. Nr.: 346721-50-4
Formel: C₂₀H₁₈N₂O₃
Molecular Weight:334.37

Speicherung:

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

XS-060 Chemical Structure

CAS. Nr.: 346721-50-4

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Preis

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Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RXRα (Retinoid X receptor alpha)^[1]

Alle RAR/RXR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	>30 μM Compound: S19	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs	[PMID: 31610376]
MDA-MB-231	IC₅₀	6.88 μM Compound: XS-060	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37058970]

In Vitro

XS-060 targeting the RXRα′ s coactivator binding site can inhibit pRXRα-PLK1 interaction and exhibits good antitumor activity as an anti-mitotic agent^[1].
XS-060 shows anti-proliferative activity against MDA-MB 231 cancer cells, with an IC₅₀ of 6.880 ± 0.059 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB 231, A549, and HepG2
Concentration:

5 μM
Incubation Time:
Result:

Showed anti-proliferative activity at 5 μM against cancer cells (MDA-MB 231, A549, and HepG2), with cell viability rate (%) of 51.93 ± 4.32, 82.65 ± 2.84, and 48.65 ± 6.45, respectively.

In Vivo

XS-060 (25 mg/kg, IP or PO, once) displays good absorption by intraperitoneal injection, but oral absorption is very poor^[1].

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

Animal Model:

Sprague-Dawley rats (10-14 weeks, 200-220g)^[1]
Dosage:

25 mg/kg
Administration:

Oral absorption (p.o.) and intraperitoneal injection (i.p.), once, (Pharmacokinetic Analysis)

Result:

The oral absorption of XS-060 is very poor, while intraperitoneal injection displayed good absorption^[1].
Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats^[1].

	XS060 25 mg/kg (i.p.)
T_max (h)	2.67 ± 1.12
C_max (μg/L)	1061.50 ± 399.20
AUC_0-∞ (μg⋅h/L)	7040.30 ± 1593.52
T_1/2 (h)	2.13 ± 0.05
CLz/F (L/(h⋅kg))	3.67 ± 0.81
Vd, z/F (L/kg)	11.31 ± 2.71

Chemical Information

CAS. Nr. 346721-50-4
Appearance Solid
Molecular Weight 334.37
Formel C₂₀H₁₈N₂O₃
Color Off-white to yellow
SMILES

COC(C=C1)=CC=C1CC(N/N=C/C2=C(O)C=CC3=C2C=CC=C3)=O
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 : 175 mg/mL (523.37 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

2.9907 mL

14.9535 mL

29.9070 mL

5 mM

0.5981 mL

2.9907 mL

5.9814 mL

10 mM

0.2991 mL

1.4953 mL

2.9907 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Chen J, et al. Discovery of bipyridine amide derivatives targeting pRXRα-PLK1 interaction for anticancer therapy. Eur J Med Chem. 2023 Apr 6;254:115341. [Content Brief]

[2]. Xie G, et al. Centrosomal Localization of RXRα Promotes PLK1 Activation and Mitotic Progression and Constitutes a Tumor Vulnerability. Dev Cell. 2020 Dec 21;55(6):707-722.e9. [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	2.9907 mL	14.9535 mL	29.9070 mL	74.7675 mL
	5 mM	0.5981 mL	2.9907 mL	5.9814 mL	14.9535 mL
	10 mM	0.2991 mL	1.4953 mL	2.9907 mL	7.4767 mL
	15 mM	0.1994 mL	0.9969 mL	1.9938 mL	4.9845 mL
	20 mM	0.1495 mL	0.7477 mL	1.4953 mL	3.7384 mL
	25 mM	0.1196 mL	0.5981 mL	1.1963 mL	2.9907 mL
	30 mM	0.0997 mL	0.4984 mL	0.9969 mL	2.4922 mL
	40 mM	0.0748 mL	0.3738 mL	0.7477 mL	1.8692 mL
	50 mM	0.0598 mL	0.2991 mL	0.5981 mL	1.4953 mL
	60 mM	0.0498 mL	0.2492 mL	0.4984 mL	1.2461 mL
	80 mM	0.0374 mL	0.1869 mL	0.3738 mL	0.9346 mL
	100 mM	0.0299 mL	0.1495 mL	0.2991 mL	0.7477 mL

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

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

Produktname:
Art. -Nr.:
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XS-060

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Protein-protein Interaction Inhibitor Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive 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

XS-060

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Protein-protein Interaction Inhibitor Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive 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

XS-060 Related Classifications

HY-149085 Related Classifications