NU7441
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MedKoo CAT#: 406320

CAS#: 503468-95-9

Description: NU7441, also known as KU-57788, is a highly potent and selective DNA-PK inhibitor (IC50=14 nM), exhibiting ATP-competitive inhibition kinetics. NU7441 increased the cytotoxicity of ionizing radiation and etoposide in SW620, LoVo, and V3-YAC cells but not in V3 cells, confirming that potentiation was due to DNA-PK inhibition. NU7441 substantially retarded the repair of ionizing radiation-induced and etoposide-induced DSB.


Chemical Structure

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NU7441
CAS# 503468-95-9

Theoretical Analysis

MedKoo Cat#: 406320
Name: NU7441
CAS#: 503468-95-9
Chemical Formula: C25H19NO3S
Exact Mass: 413.10856
Molecular Weight: 413.49
Elemental Analysis: C, 72.62; H, 4.63; N, 3.39; O, 11.61; S, 7.75

Price and Availability

Size Price Availability Quantity
10.0mg USD 120.0 Ready to ship
25.0mg USD 190.0 Ready to ship
50.0mg USD 350.0 Ready to ship
100.0mg USD 550.0 Ready to ship
200.0mg USD 1050.0 Ready to ship
500.0mg USD 2250.0 Ready to ship
1.0g USD 3250.0 Ready to ship
Bulk inquiry

Synonym: NU7441; NU-7441; NU 7441; KU-57788; KU 57788; KU57788

IUPAC/Chemical Name: 8-(4-dibenzothienyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one

InChi Key: JAMULYFATHSZJM-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H19NO3S/c27-21-15-23(26-11-13-28-14-12-26)29-24-17(6-3-9-20(21)24)19-8-4-7-18-16-5-1-2-10-22(16)30-25(18)19/h1-10,15H,11-14H2

SMILES Code: O=C1C=C(N2CCOCC2)OC3=C(C4=C5C(C6=CC=CC=C6S5)=CC=C4)C=CC=C13

Appearance: Off-white to beige solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly.

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: KU-57788 (NU7441) is a DNA-PK inhibitor with an IC50 of 14 nM.
In vitro activity: The effect of NU7441 on the growth of liver cancer HepG2 cells treated with different doses of NU7441, from 0.5 to 10 µM was investigated (Fig. 1). NU7441 had an inhibitory effect on cell growth, indicating the potential application of this medicine to kill the cancer cells. Moreover, this inhibition was dose- and time-dependent, with a maximal inhibitory effect for 72 h at a dosage of 10 µM NU7441. Reference: Cell Physiol Biochem. 2016;38(5):1897-905. https://www.karger.com/Article/FullText/445551
In vivo activity: Mice bearing SW620 tumor xenografts were treated with etoposide phosphate alone and in combination with NU7441 ( Fig. 5B). Tumors in control mice reached four times their starting volume (RTV4) at a median time of 5.6 days (i.e., time to RTV4 = 5.6 days). Treatment with etoposide phosphate alone caused a tumor growth delay of 2.7 days (time to RTV4 = 8.3 days), which was extended to 5.4 days (time to RTV4 = 11 days, P = 0.0159 compared with etoposide alone) by coadministration of NU7441. Thus, NU7441 enhanced etoposide phosphate efficacy by 100%. Reference: Cancer Res. 2006 May 15;66(10):5354-62. https://cancerres.aacrjournals.org/content/66/10/5354.long

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 14.0 33.9

Preparing Stock Solutions

The following data is based on the product molecular weight 413.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Yang C, Wang Q, Liu X, Cheng X, Jiang X, Zhang Y, Feng Z, Zhou P. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905. doi: 10.1159/000445551. Epub 2016 May 9. PMID: 27160694. 2. Zhao Y, Thomas HD, Batey MA, Cowell IG, Richardson CJ, Griffin RJ, Calvert AH, Newell DR, Smith GC, Curtin NJ. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 2006 May 15;66(10):5354-62. doi: 10.1158/0008-5472.CAN-05-4275. PMID: 16707462.
In vitro protocol: 1. Yang C, Wang Q, Liu X, Cheng X, Jiang X, Zhang Y, Feng Z, Zhou P. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905. doi: 10.1159/000445551. Epub 2016 May 9. PMID: 27160694.
In vivo protocol: 1. Zhao Y, Thomas HD, Batey MA, Cowell IG, Richardson CJ, Griffin RJ, Calvert AH, Newell DR, Smith GC, Curtin NJ. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 2006 May 15;66(10):5354-62. doi: 10.1158/0008-5472.CAN-05-4275. PMID: 16707462.

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1: Tichy A, Durisova K, Salovska B, Pejchal J, Zarybnicka L, Vavrova J, Dye NA, Sinkorova Z. Radio-sensitization of human leukaemic MOLT-4 cells by DNA-dependent protein kinase inhibitor, NU7441. Radiat Environ Biophys. 2013 Oct 8. [Epub ahead of print] PubMed PMID: 24100951.

2: Tavecchio M, Munck JM, Cano C, Newell DR, Curtin NJ. Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination. Cancer Chemother Pharmacol. 2012 Jan;69(1):155-64. doi: 10.1007/s00280-011-1662-4. Epub 2011 Jun 1. PubMed PMID: 21630086.

3: Zhao Y, Thomas HD, Batey MA, Cowell IG, Richardson CJ, Griffin RJ, Calvert AH, Newell DR, Smith GC, Curtin NJ. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 2006 May 15;66(10):5354-62. PubMed PMID: 16707462.

4: Leahy JJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GC. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. PubMed PMID: 15546735.

NU7441

10.0mg / USD 120.0


Additional Information