AMXT-1501 tetrahydrochloride|西域试剂

AMXT-1501 tetrahydrochloride,98.0%

产品编号：Bellancom-124617A| 分子式：C₃₂H₇₂Cl₄N₆O₂| 分子量：714.77

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-124617A	￥5500.00	杭州北京（现货）
Bellancom-124617A	￥8500.00	杭州北京（现货）
Bellancom-124617A	￥18500.00	杭州北京（现货）
Bellancom-124617A	￥28500.00	杭州北京（现货）

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AMXT-1501 tetrahydrochloride

产品介绍

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 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.

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

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
(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.

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

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.

体内研究

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

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.

体内研究

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

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.

性状

Solid

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 (sealed storage, away from moisture and 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。

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