AMXT-1501 tetrahydrochloride,2

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AMXT-1501 tetrahydrochloride

CAS No. :

MCE 国际站：AMXT-1501 tetrahydrochloride

产品活性：AMXT-1501 tetrahydrochloride 是一种具有口服活性的多胺转运系统 (polyamine transport) 抑制剂。AMXT-1501 可阻断免疫活性小鼠中的肿瘤生长，但不能阻断缺乏 T 细胞无胸腺裸鼠中的肿瘤生长。DFMO 和 AMXT-1501 联合诱导 caspase-3 介导的 NB 细胞凋亡。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: AMXT-1501 tetrahydrochloride (0.39-50 µM; 48 hours) treatment exhibits cytotoxicity against this panel of NB cell lines (BE(2)-C, SMS-KCNR and SH-SY5Y cells), with IC₅₀ values of 17.72 µM for SMS-KCNR, 17.69 µM for BE(2)-C, and 14.13 µM for SH-SY5Y.
BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells are exposed to AMXT-1501 tetrahydrochloride (2.5 µM) and DFMO (2.5 mM) alone or in combination (AMXT-1501 tetrahydrochloride 2.5 µM + DFMO 2.5 mM). After 96 hours exposure to AMXT-1501 tetrahydrochloride or DFMO does not significantly alter the level of noncleaved PARP, cleaved PARP and cleaved caspase 3, whereas cells treated with the combination of AMXT-1501 tetrahydrochloride with DFMO decrease the amount of noncleaved PARP and increase the amount of cleaved PARP and cleaved caspase 3.

In Vivo: AMXT-1501 tetrahydrochloride (3 mg/kg; subcutaneous injection; every day; 28 days) alone is sufficient to delay EAE onset moderately,but fails to protect animals from reaching the endpoint. However, the combination of DFMO and AMXT-1501 tetrahydrochloride are sufficient to deplete T cell polyamine pool, and consequently suppress T cell proliferation and effector function in vivo.

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