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。

AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.

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Polyamine transport

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. has not independently confirmed the

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. Candace S Hayes, et al. Polyamine-blocking therapy reverses immunosuppression in the tumor microenvironment. Cancer Immunol Res. 2014 Mar;2(3):274-85.
[2]. Katherine Samal, et al. AMXT‐1501, a novel polyamine transport inhibitor, synergizes with DFMO in inhibiting neuroblastoma cell proliferation by targeting both ornithine decarboxylase and polyamine transport. Int J Cancer. 2013 Sep 15;133(6):1323-33.

In Vitro: H₂O : 83.33 mg/mL (116.58 mM; Need ultrasonic)配制储备液