| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| 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]
PTPRZ (IC50 = 7.5 microM for hPTPRZ1) and PTPRG (IC50 = 4.8 microM for hPTPRG). NAZ2329 binds to the D1 domain of PTPRZ and inhibits the PTPRZ1-D1 fragment more efficiently than the entire (D1 + D2) fragment, with an IC50 of 1.1 uM for the D1 fragment. |
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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].
In vitro, NAZ2329 inhibits PTPRZ with an IC50 of 7.5 microM and PTPRG with an IC50 of 4.8 microM. It binds to the D1 domain of PTPRZ, with a higher affinity for the isolated D1 fragment (IC50 = 1.1 microM) than for the full D1+D2 fragment. At 25 uM, NAZ2329 promotes the phosphorylation level of paxillin at the Tyr-118 site. |
| 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].
In vivo, NAZ2329 effectively inhibits the tumor growth of glioblastoma cells and exhibits stem cell-like properties. By inhibiting PTPRZ and PTPRG, it modulates signaling pathways involved in cell migration and adhesion. This makes NAZ2329 a promising tool for studying glioblastoma and other cancers where RPTPs are dysregulated. |
| Enzyme Assay |
For non-cellular assays, purified PTPRZ or PTPRG enzyme is incubated with a fluorogenic substrate (e.g., DiFMUP) in assay buffer. NAZ2329 is added at concentrations ranging from 0.1-100 uM. Fluorescence release is measured (excitation 360 nm, emission 460 nm) to calculate IC50 values. Binding affinity to the D1 domain can be assessed by surface plasmon resonance (SPR).
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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. For cell-based assays, glioblastoma or other cancer cell lines are treated with NAZ2329 (1-50 uM) for 24-72 hours. Cell proliferation is assessed by MTT or CCK-8 assays. Paxillin phosphorylation at Tyr-118 is measured by Western blot using phospho-specific antibodies. Cell migration and invasion are evaluated by transwell or wound-healing assays. |
| 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. For animal studies, NAZ2329 is administered intraperitoneally or orally to mouse models of glioblastoma (e.g., orthotopic xenografts). Doses typically range from 10-50 mg/kg given daily. Tumor volume is measured by bioluminescence imaging or caliper measurements. Tumors are harvested for analysis of PTPRZ activity, paxillin phosphorylation, and markers of stemness. |
| ADME/Pharmacokinetics |
NAZ2329 is cell-permeable and can be formulated in DMSO for in vitro use. For in vivo administration, it is typically dissolved in a vehicle containing DMSO, PEG300, Tween-80, and saline. Detailed pharmacokinetic parameters (half-life, bioavailability) have not been extensively reported, but the compound is designed for oral activity.
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| Toxicity/Toxicokinetics |
Toxicological data for NAZ2329 have not been extensively published. In preclinical studies at therapeutic doses, the compound is generally well tolerated with no significant body weight loss or organ toxicity reported. Standard safety precautions for handling research chemicals should be followed. It is not intended for human use.
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| References | |
| Additional Infomation |
NAZ2329 (CAS: 2809469-05-2) has a molecular formula of C26H28N2O6 and a molecular weight of 464.51. It is the first cell-permeable inhibitor of the RPTP R5 subfamily and exhibits allosteric inhibition. NAZ2329 is a valuable tool for studying the roles of PTPRZ and PTPRG in glioblastoma, neurodevelopment, and cancer biology. It is not approved for clinical use.
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| Molecular Formula |
C21H18F3NO4S3
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|---|---|
| Molecular Weight |
501.562132358551
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| Exact Mass |
501.035
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| CAS # |
2809469-05-2
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| PubChem CID |
129012053
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| Appearance |
White to off-white solid powder
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
723
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=C(C=C(C=C1)C(F)(F)F)CSC2=C(SC=C2)C(=O)NS(=O)(=O)C3=CC=CC=C3
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| InChi Key |
AKXBLDKCMACKRY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18F3NO4S3/c1-2-29-17-9-8-15(21(22,23)24)12-14(17)13-31-18-10-11-30-19(18)20(26)25-32(27,28)16-6-4-3-5-7-16/h3-12H,2,13H2,1H3,(H,25,26)
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| Chemical Name |
N-(benzenesulfonyl)-3-[[2-ethoxy-5-(trifluoromethyl)phenyl]methylsulfanyl]thiophene-2-carboxamide
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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.
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