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。
| 生物活性 | AMXT-1501 tetrahydrochloride is an orally activepolyamine transportinhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells[1]. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediatedapoptosisin NB cell lines[2]. |
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体外研究
(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 IC50values of 17.72 μM for SMS-KCNR, 17.69 μM for BE(2)-C, and 14.13 μM for SH-SY5Y[2].
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[2].
Cell Viability Assay[2] | Cell Line: | BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells | | Concentration: | 0.39 μM, 1 μM, 3.1 μM, 10 μM, 31 μM, 50 μM | | Incubation Time: | 48 hours | | Result: | AMXT-1501 tetrahydrochloride exhibited cytotoxicity against this panel of NB cell lines. |
Western Blot Analysis[2] | Cell Line: | BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells | | Concentration: | 2.5 μM | | Incubation Time: | 72 hours | | Result: | Combination treatment with DFMO decreased the amount of noncleaved PARP and increased the amount of cleaved PARP and cleaved caspase 3 in all three cell lines. |
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体内研究
(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[3].
| Animal Model: | C57BL/6 (WT) andODCknockout strain (ODCcKO) mice bearing experimental autoimmune encephalomyelitis (EAE) model[3] | | Dosage: | 3 mg/kg | | Administration: | Subcutaneous injection; every day; 28 days | | Result: | Displayed a delayed disease onset initially, but eventually proceeded with pathologic development and reached the endpoint. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 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) |
| 溶解性数据 | In Vitro: H2O : 83.33 mg/mL(116.58 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.3991 mL | 6.9953 mL | 13.9905 mL | | 5 mM | 0.2798 mL | 1.3991 mL | 2.7981 mL | | 10 mM | 0.1399 mL | 0.6995 mL | 1.3991 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 50 mg/mL (69.95 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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