AMXT-1501 tetrahydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AMXT-1501 tetrahydrochloride  纯度: ≥98.0%

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

AMXT-1501 tetrahydrochloride Chemical Structure

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥8500 In-stock
25 mg ￥18500 In-stock
50 mg ￥28500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

AMXT-1501 tetrahydrochloride 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Orally Active Compound Library

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[1]. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines[2].

IC50 & Target

Polyamine transport[1]
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 IC50 values 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 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 [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.

Clinical Trial

分子量

714.77

Formula

C32H72Cl4N6O2
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
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。
参考文献

  • [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.

    [3]. Ruohan Wu, et al. De novo synthesis and salvage pathway coordinately regulate polyamine homeostasis and determine T cell proliferation and function. Sci Adv. 2020 Dec 16;6(51):eabc4275.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务