Art. -Nr.: HY-123611

Supinoxin

(Synonyms: RX-5902)

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Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC₅₀s ranging from 10 nM to 20 nM.

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Reinheit: 99.67%
CAS. Nr.: 888478-45-3
Formel: C₂₂H₂₄FN₅O₄
Molecular Weight:441.46

Speicherung:

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

Supinoxin Chemical Structure

CAS. Nr.: 888478-45-3

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Helicase

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.021 μM Compound: 25	Growth inhibition of human A549 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human A549 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
CAKI-1	IC₅₀	0.011 μM Compound: 25	Growth inhibition of human Caki1 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human Caki1 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
HCT-116	IC₅₀	0.02 μM Compound: 25	Growth inhibition of human HCT116 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human HCT116 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
HCT-15	IC₅₀	21 nM Compound: 25	Growth inhibition of human HCT15 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human HCT15 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
HeLa	IC₅₀	0.021 μM Compound: 25	Growth inhibition of human HeLa cells after 96 hrs by sulforhodamine B assay Growth inhibition of human HeLa cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
HepG2	IC₅₀	0.019 μM Compound: 25	Growth inhibition of human HepG2 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human HepG2 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
HT-29	IC₅₀	0.021 μM Compound: 25	Growth inhibition of human HT-29 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human HT-29 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
MDA-MB-231	IC₅₀	0.012 μM Compound: 25	Growth inhibition of human MDA-MB-231 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-231 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
MKN-45	IC₅₀	0.02 μM Compound: 25	Growth inhibition of human MKN45 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human MKN45 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
OVCAR-3	IC₅₀	0.012 μM Compound: 25	Growth inhibition of human OVCAR-3 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human OVCAR-3 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
PANC-1	IC₅₀	0.021 μM Compound: 25	Growth inhibition of human PANC1 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human PANC1 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
PC-3	IC₅₀	0.021 μM Compound: 25	Growth inhibition of human PC3 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human PC3 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
SK-MEL-28	IC₅₀	0.02 μM Compound: 25	Growth inhibition of human SK-MEL-28 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human SK-MEL-28 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]
U-251	IC₅₀	0.015 μM Compound: 25	Growth inhibition of human U251 cells after 96 hrs by sulforhodamine B assay Growth inhibition of human U251 cells after 96 hrs by sulforhodamine B assay	[PMID: 20943401]

In Vitro

RX-5902 (0-10 μM; 72 hours) is active against cell lines of all TNBC molecular subtypes and is active against cell lines with mutations in p53, RB1, CDKN2A, and loss of PTEN^[1].
RX-5902 (20-100 nM; 24 hours) treatment results in a dose-dependent increase in tetraploid cells, consistent with induction of G2–M cell-cycle arrest^[1].
RX-5902 (0-100 nM; 72 hours) exhibits no significant induction of apoptosis in cell lines resistant to the antiproliferative effects of RX5902. But in sensitive cells, the observed activation of apoptosis begins at 24–48 hours and reaches a peak at 72 hours. The induced apoptosis is greasted with a dose of 100 nM^[1].
RX-5902 (0-100 nM; 24 or 48 hours) decreases MCL-1 expression as a dose-dependent manner in TNBC cell lines sensitive to RX-5902^[1].
RX-5902 inhibits cell growth, MDA-MB-231, Caki-1, UMRC2, PANC-1, A549, MKN-45, HepG2, HCT116, HT29, PC-3, U251, HeLa, SK-MEL-28 and OVCAR-3 with IC₅₀ values range from 0.01 μM to 0.021 μM in the growth inhibition of cancer cells^[2].

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

Cell Viability Assay^[1]

Cell Line:

MDA-MB-231, HCC1806, Hs578t, CAL-85-1, HCC38, HCC1187, MDA-MB-436, CAL-51, HCC38, BT549, MDAMB-157, HDQ-P1, HCC1395, MDA-MB-436, HCC1937, CAL-120, BT20 cells
Concentration:

0-10 μM
Incubation Time:

72 hours
Result:

Displayed the average IC₅₀ of the cell lines sensitive to RX-5902 treatment is 56 nM.

Cell Cycle Analysis^[1]

Cell Line:

Sensitive (MDA-MB-231 and HCT1806) and two resistant (MDA-MB-436 and CAL-120) cell lines
Concentration:

20 nM; 100 nM
Incubation Time:

24 hours
Result:

Led to G2-M cell-cycle arrest at sensitive cells.

Apoptosis Analysis^[1]

Cell Line:

Sensitive (MDA-MB-231 and HCT1806) and two resistant (MDA-MB-436 and CAL-120) cell lines
Concentration:

0-100 nM
Incubation Time:

24-72 hours
Result:

Induced cell apoptosis in sensitive cell lines and peaks at 72 hours.

Western Blot Analysis^[1]

Cell Line:

Cal-51, HCC-1806, and MDA-MB-468 cells
Concentration:

20 nM; 100 nM
Incubation Time:

24 hours
Result:

Induced inhibition of MCL-1 expression in Cal-51, HCC-1806, and MDA-MB-468 cells.

In Vivo

RX-5902 (oral administration; 160/320/600 mg/kg; once weekly for 3 weeks) significant dose-dependent tumor growth inhibition (TGI) in the MDA-MB-231 model, exhibits TGI of 55.7%, 80.29% and 94.58% at 160 mg/kg, 320 mg/kg and 600 mg/kg, respectively. It is more efficacious than the chemotherapy control arm of nab-paclitaxel (TGI 45%)^[1].

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

Animal Model:

MDAMD-231 xenograft model in mice^[1]
Dosage:

160 mg/kg; 320 mg/kg; 600 mg/kg
Administration:

Oral administration; once weekly for 3 weeks
Result:

Decreased tumor volume as a dose-dependent manner.

Clinical Trial

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

Chemical Information

CAS. Nr. 888478-45-3
Appearance Solid
Molecular Weight 441.46
Formel C₂₂H₂₄FN₅O₄
Color White to off-white
SMILES

O=C(N1CCN(C2=CC(OC)=CC(OC)=C2)CC1)NC3=NC4=CC(F)=CC=C4N=C3OC
Synonyms

RX-5902
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 (226.52 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

2.2652 mL

11.3261 mL

22.6521 mL

5 mM

0.4530 mL

2.2652 mL

4.5304 mL

10 mM

0.2265 mL

1.1326 mL

2.2652 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Kost GC, et al. A Novel Anti-Cancer Agent, 1-(3,5-Dimethoxyphenyl)-4-[(6-Fluoro-2-Methoxyquinoxalin-3-yl)Aminocarbonyl] Piperazine (RX-5902), Interferes With β-Catenin Function Through Y593 Phospho-p68 RNA Helicase.J Cell Biochem. 2015 Aug;116(8):1595-601. [Content Brief]

[2]. Capasso A, et al. First-in-Class Phosphorylated-p68 Inhibitor RX-5902 Inhibits β-Catenin Signaling and Demonstrates Antitumor Activity in Triple-Negative Breast Cancer.Nov;18(11):1916-1925. [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	2.2652 mL	11.3261 mL	22.6521 mL	56.6303 mL
	5 mM	0.4530 mL	2.2652 mL	4.5304 mL	11.3261 mL
	10 mM	0.2265 mL	1.1326 mL	2.2652 mL	5.6630 mL
	15 mM	0.1510 mL	0.7551 mL	1.5101 mL	3.7754 mL
	20 mM	0.1133 mL	0.5663 mL	1.1326 mL	2.8315 mL
	25 mM	0.0906 mL	0.4530 mL	0.9061 mL	2.2652 mL
	30 mM	0.0755 mL	0.3775 mL	0.7551 mL	1.8877 mL
	40 mM	0.0566 mL	0.2832 mL	0.5663 mL	1.4158 mL
	50 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1326 mL
	60 mM	0.0378 mL	0.1888 mL	0.3775 mL	0.9438 mL
	80 mM	0.0283 mL	0.1416 mL	0.2832 mL	0.7079 mL
	100 mM	0.0227 mL	0.1133 mL	0.2265 mL	0.5663 mL

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Supinoxin

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Supinoxin

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Supinoxin Related Classifications

HY-123611 Related Classifications