AMXT-1501 tetrahydrochloride

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目录号 : KM3013

Data Sheet 产品使用指南

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。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

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.

体外研究

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.

Cell Viability Assay

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

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.

体内研究

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.

Animal Model:	C57BL/6 (WT) and ODC knockout strain (ODC cKO) mice bearing experimental autoimmune encephalomyelitis (EAE) model
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.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

H₂O : 83.33 mg/mL (116.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

临床试验