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NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 μM for hPTPRZ1) and PTPRG (IC50=4.8 μM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 μM) than the whole intracellular (D1?+?D2) fragment (IC50 of 7.5 μM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties[1]. | [in vivo]
NAZ2329 (22.5 mg/kg; intraperitoneal injection; twice per week; 40 days) alone? has a moderate inhibitory effect. However, the combination of Temozolomide and NAZ2329 exerts a significantly increased inhibition of tumor growth compared with the control group, the NAZ2329 monotherapy group and the Temozolomide monotherapy group[1]. | Animal Model: | Female BALB/c- nu/nu mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells[1] | | Dosage: | 22.5?mg/kg; Temozolomide (TMZ, 50?mg/kg) | | Administration: | Intraperitoneal injection; twice per week; 40 days | | Result: | The combination of NAZ2329 and TMZ significantly 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. DOI:10.1038/s41598-017-05931-8 |
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