Art. -Nr.: HY-18768

NCT-501

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

NCT-501 is a reversible, non-competitive, selective, blood-brain barrier-permeable ALDH1A1 inhibitor with an IC₅₀ of 40 nM. NCT-501 inhibits the AKT-β-catenin signaling pathway, induces necroptosis in nasopharyngeal carcinoma cells, suppresses their proliferation and inhibits stem cell spheroid formation. NCT-501 can be used in research related to nasopharyngeal carcinoma, esophageal squamous cell carcinoma and malignant tumors.

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Reinheit: 99.59%
CAS. Nr.: 1802088-50-1
Formel: C₂₁H₃₂N₆O₃
Molecular Weight:416.52

Speicherung:

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

NCT-501 Chemical Structure

CAS. Nr.: 1802088-50-1

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

ALDH1

Alle Aldehyde Dehydrogenase (ALDH) Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
OV-90	EC₅₀	43.9 μM Compound: 4	Cytotoxicity against 3D culture of human OV90 cells assessed as decrease in cell viability after 6 days by CellTiter-Glo assay Cytotoxicity against 3D culture of human OV90 cells assessed as decrease in cell viability after 6 days by CellTiter-Glo assay	[PMID: 29767973]

In Vitro

NCT-501 inhibits stem cell spheroid formation in human nasopharyngeal carcinoma SUNE1 cells^[1].
NCT-501 (5 days) reduces cell viability in human nasopharyngeal carcinoma 5-8F, 6-10B, SUNE1, and HK1 cells with IC₅₀ values of 96.91 μM, 64.15 μM, 27.84 μM, and 67.97 μM respectively, with greater sensitivity in cells with higher ALDH1A1 expression^[1].
NCT-501 (14 days) inhibits colony formation in human nasopharyngeal carcinoma 6-10B and SUNE1 cells^[1].
NCT-501 induces necroptosis in human nasopharyngeal carcinoma SUNE1 cells, as evidenced by caspase-independent cell death, characteristic nuclear and ultrastructural changes, and HMGB1 translocation^[1].
NCT-501 downregulates ALDH1A1 expression and inhibits components of the AKT-β-catenin signaling pathway in TE-1 esophageal squamous cell carcinoma cells, with significant reductions in ALDH1A1 and AKT1 protein levels to ~0.4 relative to β-actin^[2].

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

Parmacokinetics

Species	Dose	Route	C_max	T_1/2 (Plasma)	AUC_0-24	Bioavailability	C_max (Brain)	T_1/2 (Brain)	T_1/2	V_ss	CL
Mice^[3]	2 mg/kg	i.v.	2070 ng/mL	/	332 ng·h/mL	/	/	/	0.5 h	1.8 L/kg	98 mL/min/kg
Mice^[3]	30 mg/kg	i.p.	8080 ng/mL	/	5670 ng·h/mL	100 %	/	/	0.7 h	/	/
Mice^[3]	10 mg/kg	p.o.	696 ng/mL	0.4 h	484 ng·h/mL	29 %	1130 ng/mL	0.4 h	/	/	/

In Vivo

Animal Model:

5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells)^[1]
Dosage:

100µg/animal
Administration:

Intra-tumorally (i.t); every alternate day for 20 days
Result:

Showed a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts.

Chemical Information

CAS. Nr. 1802088-50-1
Appearance Solid
Molecular Weight 416.52
Formel C₂₁H₃₂N₆O₃
Color White to off-white
SMILES

O=C(N1C)N(C)C2=C(N(CCC(C)C)C(CN3CCN(C(C4CC4)=O)CC3)=N2)C1=O
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

Publications (5)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyIn Vivo Imaging

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Journal Impact Factor

Free Radical Bio Med

Disulfiram suppresses NLRP3 inflammasome activation to treat peritoneal and gouty inflammation. [Abstract]

2020 May 20;152:8-17. PMID: 32151746
Mol Cancer Ther

ALDH1A1 Contributes to PARP Inhibitor Resistance via Enhancing DNA Repair in BRCA2-/- Ovarian Cancer Cells. [Abstract]

2020 Jan;19(1):199-210. PMID: 31534014

NCT-501 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Jan;19(1):199-210. [Abstract]

The ALDH1A1 inhibitor NCT-501 synergistically augments the cytotoxicity of olaparib in BRCA2-deficient EOC cell lines. PEO1 and Kuramochi cells were treated with olaparib, NCT-501, or olaparib+NCT-501 for 7 days, cell viability was determined using the methylene blue assay.

NCT-501 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Jan;19(1):199-210. [Abstract]

PEO1-R cells (2 × 10⁶) were injected into nude mice subcutaneously to generate xenografts, treated with olaparib (50 mg/kg, once a day) or/and NCT-501 (10 mg/kg, once a day) intraperitoneally for 8 days. Tumor volumes were determined using caliber every other day.

NCT-501 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Jan;19(1):199-210. [Abstract]

PEO1 cells containing luciferase expression vector (2 × 10⁶) were injected into nude mice intraperitoneally to generate xenografts, treated with olaparib (50 mg/kg, once a day) or/and NCT-501 (10 mg/kg, once a day) intraperitoneally for 10 days. Tumor volumes were determined using BLI.
iScience

Development of retinoid nuclear receptor pathway antagonists through targeting aldehyde dehydrogenase 1A3. [Abstract]

2025 Oct 3;28(11):113675. PMID: 41210994
Mol Carcinog

Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by aldehyde dehydrogenase 1 A1 inhibition. [Abstract]

2017 Feb;56(2):694-711. PMID: 27380877
Research Square Preprint

2023 Jul 21.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 3.57 mg/mL (8.57 mM; ultrasonic and warming and heat to 60°C; 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

2.4008 mL

12.0042 mL

24.0085 mL

5 mM

0.4802 mL

2.4008 mL

4.8017 mL

10 mM

---

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (3.00 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.00 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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 (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]. Wang H, et al. Targeting ALDH1A1 to induce Necroptosis in Nasopharyngeal Carcinoma. J Cancer. 2022;13(14):3515-3525. Published 2022 Oct 24. [Content Brief]

[2]. Wang W, et al. ALDH1A1 maintains the cancer stem-like cells properties of esophageal squamous cell carcinoma by activating the AKT signal pathway and interacting with β-catenin. Biomed Pharmacother. 2020;125:109940. [Content Brief]

[3]. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-78.
[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	2.4008 mL	12.0042 mL	24.0085 mL	60.0211 mL
DMSO	5 mM	0.4802 mL	2.4008 mL	4.8017 mL	12.0042 mL

NCT-501

5 Cited Publications

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NCT-501

Kinase Inhibitor Library

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Targeted Diversity Library

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Anti-Prostate Cancer Compound Library

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Cancer Stem Cells Compound Library

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Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

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Anti-Ovarian Cancer Compound Library

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Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) NCT-501

Alle Aldehyde Dehydrogenase (ALDH) Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NCT-501 Related Classifications

HY-18768 Related Classifications