Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 7.5 µM (PTPRZ), 4.8 µM (PTPRG), 35.7 µM (PTPRA), 56.7 µM (PTPRM), 23.7 µM (PTPRS), 35.4 µM (PTPRB), 15.2 µM (PTPN6), 14.5 µM (PTPN1)[1]
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ln Vitro |
In all cell lines (rat glioblastoma cells harboring C6 clone and human U251 glioblastoma cells), NAZ2329 (0-25 μM; 48 hours) inhibits cell proliferation and migration in a dose-dependent manner[1]. By considerably increasing the phosphorylation level of the paxillin Tyr-118 site, NAZ2329 (25 μM; 0-90 min) inhibits PTPR substrates [1].
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ln Vivo |
The single dose of NAZ2329 (22.5 mg/kg; i.p.; twice weekly; 40 days) was only somewhat inhibitive. However, the combination of temozolomide and NAZ2329 significantly increased the inhibitory effect of temozolomide on tumor growth when compared to the control group, NAZ2329 single-drug treatment group, and temozolomide single-drug treatment group[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Rat glioblastoma cells bearing C6 clone, human U251 glioblastoma cells Tested Concentrations: 0 µM, 6.3 µM, 12.5 µM, 25 µM Incubation Duration: 48 hrs (hours) Experimental Results: Exerted inhibition in cell proliferation and migration in a dose -dependent manner. Western Blot Analysis[1] Cell Types: Rat glioblastoma cells bearing C6 clone Tested Concentrations: 25 µM Incubation Duration: 0 min, 15 min, 30 min, 60 min, 90min Experimental Results: Promoted the phosphorylation level of paxillin at Tyr- 118 sites. |
Animal Protocol |
Animal/Disease Models: Female BALB/c- nu/nu (nude) mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells[1]
Doses: 22.5 mg/kg; Temozolomide (TMZ, 50 mg/kg) Route of Administration: intraperitoneal (ip) injection; twice per week; 40 days Experimental Results: The combination of NAZ2329 and TMZ Dramatically delayed tumor growth compared to NAZ2329 or TMZ alone. |
References |
[1]. Akihiro Fujikawa, et al. Targeting PTPRZ inhibits stem cell-like properties and tumorigenicity in glioblastoma cells. Sci Rep. 2017 Jul 17;7(1):5609.
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Molecular Formula |
C21H18F3NO4S3
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Molecular Weight |
501.56
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CAS # |
2809469-05-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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: 100 mg/mL (199.38 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.98 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9938 mL | 9.9689 mL | 19.9378 mL | |
5 mM | 0.3988 mL | 1.9938 mL | 3.9876 mL | |
10 mM | 0.1994 mL | 0.9969 mL | 1.9938 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.