ASP4132|cas:1640294-30-9|西域试剂

ASP4132,98.85%

产品编号：Bellancom-136447| CAS NO：1640294-30-9| 分子式：C₄₆H₅₁F₃N₆O₈S₂| 分子量：937.06

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货号	价格	库存与货期
Bellancom-136447	￥1500.00	杭州北京（现货）
Bellancom-136447	￥2500.00	杭州北京（现货）
Bellancom-136447	￥4500.00	杭州北京（现货）
Bellancom-136447	￥7500.00	杭州北京（现货）
Bellancom-136447	￥12500.00	杭州北京（现货）

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ASP4132

产品介绍

ASP4132 是一种具有口服活性，有效的 AMPK 激活剂，EC₅₀ 为 18 nM。ASP4132 具有抗癌活性，可在乳腺癌异种移植小鼠模型中促使肿瘤消退。

生物活性

ASP4132 is an orally active, potent AMPK activator with an EC₅₀ of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.

体外研究

ASP4132 shows comparable cell growth inhibitory (IC₅₀=0.014 μM) activity against MDA-MB-453 breast cancer cell.
ASP4132 shows relatively weak antiproliferative activity against SK-BR-3 (IC₅₀>3 μM).

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

体内研究

ASP4132 (0.5-8 mg/kg; PO; once daily; for 21 days) causes the tumor growth inhibition and regression.
ASP4132 (1 mg/kg; IV or PO) has a T_1/2 of 3.6 hours, a CL_tot of 19 mL/min•kg, and a V_ss of 4.6 L/kg for rats for IV.
ASP4132 is stable in human liver microsomes (HLM CL_{int, vitro}=61 mL/min•kg).

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

Animal Model:	Five-week-old male nude mice with MDA-MB-453
Dosage:	0.5, 1, 2, 4, 8 mg/kg
Administration:	PO; once daily; for 21 days
Result:	The tumor growth inhibition (TGI) rate was 29% at 1 mg/kg, and the tumor regression rate was 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively.

Animal Model:	Male SD rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 3.6 hours, a CL_tot of 19 mL/min•kg, and a V_ss of 4.6 L/kg for rats for IV. Had a C_max of 72 ng/mL and an AUC_24h of 705 ng∙h/mL for PO.

体内研究

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

Animal Model:	Five-week-old male nude mice with MDA-MB-453
Dosage:	0.5, 1, 2, 4, 8 mg/kg
Administration:	PO; once daily; for 21 days
Result:	The tumor growth inhibition (TGI) rate was 29% at 1 mg/kg, and the tumor regression rate was 26%, 87% and 96% at 2, 4 and 8 mg/kg, respectively.

Animal Model:	Male SD rats
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 3.6 hours, a CL_tot of 19 mL/min•kg, and a V_ss of 4.6 L/kg for rats for IV. Had a C_max of 72 ng/mL and an AUC_24h of 705 ng∙h/mL for PO.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (266.79 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0672 mL	5.3358 mL	10.6717 mL
5 mM	0.2134 mL	1.0672 mL	2.1343 mL
10 mM	0.1067 mL	0.5336 mL	1.0672 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)。-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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6.25 mg/mL (6.67 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (6.67 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6.25 mg/mL (6.67 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (6.67 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (6.67 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (6.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。