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MedKoo Cat#: 562387 | Name: NSC666715

Description:

WARNING: This product is for research use only, not for human or veterinary use.

NSC666715 is an inhibitor of the strand-displacement activity of DNA polymerase.

Chemical Structure

NSC666715
NSC666715
CAS#170747-33-8

Theoretical Analysis

MedKoo Cat#: 562387

Name: NSC666715

CAS#: 170747-33-8

Chemical Formula: C15H13Cl2N5O2S2

Exact Mass: 428.9888

Molecular Weight: 430.32

Elemental Analysis: C, 41.87; H, 3.05; Cl, 16.48; N, 16.28; O, 7.44; S, 14.90

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Synonym
NSC666715; NSC-666715; NSC 666715;
IUPAC/Chemical Name
4-Chloro-N-[5-(4-chloroanilino)-1H-1,2,4-triazol-3-yl]-5-methyl-2-sulfanylbenzenesulfonamide
InChi Key
GRYIAOMDOBRKIU-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H13Cl2N5O2S2/c1-8-6-13(12(25)7-11(8)17)26(23,24)22-15-19-14(20-21-15)18-10-4-2-9(16)3-5-10/h2-7,25H,1H3,(H3,18,19,20,21,22)
SMILES Code
O=S(C1=CC(C)=C(Cl)C=C1S)(NC2=NNC(NC3=CC=C(Cl)C=C3)=N2)=O
Appearance
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
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
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#A20O11B19
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
NSC666715 is an inhibitor of the strand-displacement activity of DNA polymerase.
In vitro activity:
This study examined whether NSC-666715 also blocks the dRP-lyase activity of Pol-β. The results showed inhibition of dRP-lyase activity in a dose-dependent manner with an IC50 of 4.1 μM (Fig. 2A; comparison of lane 3 with lanes 4–7, respectively). Thus, NSC-666715 appears to block dRP-lyase activity. Reference: Mol Cancer Res. 2009 Dec;7(12):1973-83. https://pubmed.ncbi.nlm.nih.gov/19996303/
In vivo activity:
These studies used SCID mouse-model for the preclinical testing of the efficacy of TMZ and NSC-666715, as described in Figure 7A. Treatment with NSC-666715 in the absence of TMZ treatment resulted in a significant decrease in the growth of xenograft tumors of all the three cell lines (37% to 54% relative to control; p<0.001) (Fig. 7B). At present, this study can propose two explanations for this effect: (i) xenograft tumors produce more abasic lesions than cells in culture, which sensitizes these cells to treatment with NSC-666715; and/or (ii) and NSC-666715 blocks critical cell survival pathways which are active in xenograft tumors but not in culture cells. Reference: Mol Cancer Res. 2009 Dec;7(12):1973-83. https://pubmed.ncbi.nlm.nih.gov/19996303/

Preparing Stock Solutions

The following data is based on the product molecular weight 430.32 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:
Jaiswal AS, Banerjee S, Panda H, Bulkin CD, Izumi T, Sarkar FH, Ostrov DA, Narayan S. A novel inhibitor of DNA polymerase beta enhances the ability of temozolomide to impair the growth of colon cancer cells. Mol Cancer Res. 2009 Dec;7(12):1973-83. doi: 10.1158/1541-7786.MCR-09-0309. Epub 2009 Dec 8. PMID: 19996303; PMCID: PMC2796282.
In vitro protocol:
Jaiswal AS, Banerjee S, Panda H, Bulkin CD, Izumi T, Sarkar FH, Ostrov DA, Narayan S. A novel inhibitor of DNA polymerase beta enhances the ability of temozolomide to impair the growth of colon cancer cells. Mol Cancer Res. 2009 Dec;7(12):1973-83. doi: 10.1158/1541-7786.MCR-09-0309. Epub 2009 Dec 8. PMID: 19996303; PMCID: PMC2796282.
In vivo protocol:
Jaiswal AS, Banerjee S, Panda H, Bulkin CD, Izumi T, Sarkar FH, Ostrov DA, Narayan S. A novel inhibitor of DNA polymerase beta enhances the ability of temozolomide to impair the growth of colon cancer cells. Mol Cancer Res. 2009 Dec;7(12):1973-83. doi: 10.1158/1541-7786.MCR-09-0309. Epub 2009 Dec 8. PMID: 19996303; PMCID: PMC2796282.
1: Jaiswal AS, Panda H, Law BK, Sharma J, Jani J, Hromas R, Narayan S. NSC666715 and Its Analogs Inhibit Strand-Displacement Activity of DNA Polymerase β and Potentiate Temozolomide-Induced DNA Damage, Senescence and Apoptosis in Colorectal Cancer Cells. PLoS One. 2015 May 1;10(5):e0123808. doi: 10.1371/journal.pone.0123808. eCollection 2015. PubMed PMID: 25933036; PubMed Central PMCID: PMC4416822.

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