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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
In HeLa cells, NSC 617145 (0.75-3 μM; 24-72 hours) exhibits WRN-specific maximum suppression of growth (98%) at the lowest concentration[1]. Protease-induced WRN binding to chromatin and proteasomal breakdown is induced by NSC 617145 (0.75 μM; 6 hours)[1]. NSC 617145 (0.125 μM) functions in concert with extremely low concentrations of Mitomycin C in FA-D2-/-cells to suppress proliferation in a way that is dependent on WRN and to cause chromosomal aberrations and double-strand breaks (DSB). In mitomycin C-treated FA-deficient cells exposed to NSC 617145, there is an increased build-up of Rad51 foci and DNA-PKcs pS2056 foci. This suggests that WRN helicase inhibition inhibits the processing of Rad51-mediated recombination products and triggers NHEJ[1]. Adult T-cell leukemia cells transformed by the human T-cell leukemia virus type 1 (HTLV-1) undergo cell cycle arrest and death when exposed to NSC 617145[2].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: HeLa cells Tested Concentrations: 0.75 μM, 1 μM, 1.5 μM, 2 μM, 3 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Inhibited cell proliferation in a WRN-specific manner. Western Blot Analysis[1] Cell Types: HeLa cells Tested Concentrations: 0.75 μM Incubation Duration: 6 hrs (hours) Experimental Results: Caused WRN to become degraded by a proteasome-mediated pathway. |
References |
[1]. Monika Aggarwal, et al. Werner syndrome helicase has a critical role in DNA damage responses in the absence of a functional fanconi anemia pathway. Cancer Res. 2013 Sep 1;73(17):5497-507.
[2]. R Moles, et al. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells. J Hematol Oncol. 2016 Nov 9;9(1):121. |
Molecular Formula |
C13H10CL4N2O4
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Molecular Weight |
400.04
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Exact Mass |
397.94
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Elemental Analysis |
C, 39.03; H, 2.52; Cl, 35.45; N, 7.00; O, 16.00
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CAS # |
203115-63-3
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Appearance |
Solid powder
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SMILES |
CC(C)(CN1C(=O)C(=C(C1=O)Cl)Cl)CN2C(=O)C(=C(C2=O)Cl)Cl
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InChi Key |
PCOXPBOKDABARQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C13H10Cl4N2O4/c1-13(2,3-18-9(20)5(14)6(15)10(18)21)4-19-11(22)7(16)8(17)12(19)23/h3-4H2,1-2H3
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Chemical Name |
3,4-dichloro-1-[3-(3,4-dichloro-2,5-dioxopyrrol-1-yl)-2,2-dimethylpropyl]pyrrole-2,5-dione
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Synonyms |
NSC 617145; NSC-617145; NSC617145
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~10 mg/mL (~25 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4998 mL | 12.4988 mL | 24.9975 mL | |
5 mM | 0.5000 mL | 2.4998 mL | 4.9995 mL | |
10 mM | 0.2500 mL | 1.2499 mL | 2.4998 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.