NCT-501 hydrochloride

Cat. No.: HY-18768A: Data Sheet Handling Instructions
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NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC₅₀ of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC₅₀ >57 μM).

For research use only. We do not sell to patients.

CAS No. : 2080306-22-3

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Other In-stock Forms of NCT-501 hydrochloride:

NCT-501

Other Forms of NCT-501 hydrochloride:

NCT-501 In-stock

5 Publications Citing Use of MCE NCT-501 hydrochloride

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

In Vivo Imaging

: NCT-501 hydrochloride 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 hydrochloride 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 hydrochloride 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.

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•Related Small Molecules:

•Related Proteins:

View All Aldehyde Dehydrogenase (ALDH) Isoform Specific Products:

View All Isoforms

ALDH1 ALDH2 ALDH3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

ALDH1

In Vitro

NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant^[1].

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

In Vivo

NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts^[1].

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

Molecular Weight

452.98

Formula

C₂₁H₃₃ClN₆O₃

CAS No.

2080306-22-3

SMILES

O=C(N1C)N(C)C2=C(N(CCC(C)C)C(CN3CCN(C(C4CC4)=O)CC3)=N2)C1=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition. [Content Brief]

[2]. 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):5967-5978. [Content Brief]