MT 63-78|cas:1179347-65-9|西域试剂

MT 63-78,98.22%

产品编号：Bellancom-W058849| CAS NO：1179347-65-9| 分子式：C₂₁H₁₄N₂O₂| 分子量：326.35

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-W058849		￥2100.00	杭州北京（现货）
Bellancom-W058849		￥3500.00	杭州北京（现货）

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MT 63-78

产品介绍

MT 63-78 是一种有效的直接 AMPK 激活剂，EC₅₀ 为 25 μM。M 63-78 还诱导细胞有丝分裂阻滞和细胞凋亡 (apoptosis)。MT 63-78 通过抑制脂肪生成和 mTORC1 途径来阻止前列腺癌的生长。MT 63-78 具有抗肿瘤作用。

生物活性

MT 63-78 is a specific and potent direct AMPK activator with an EC₅₀ of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.

体外研究

MT 63-78 (0-50 μM; 4 days; LNCaP and PC3 cells) treatment shows a dose-dependent decrease in cell number, and concomitant to the activation of AMPK signaling.
MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population.
MT 63-78 (0-50 μM; 24 hours; LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells) treatment induces reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma.
MT 63-78 (0-50 μM; 30 minutes; LNCaP and PC3 cells) treatment shows a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. And also increases Thr172 phosphorylation on the AMPK α subunit.

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

Cell Viability Assay

Cell Line:	LNCaP and PC3 cells
Concentration:	0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM
Incubation Time:	4 days
Result:	A dose-dependent decrease in cell number, concomitant to the activation of AMPK signaling was observed.

Cell Cycle Analysis

Cell Line:	LNCaP and CRPC cells
Concentration:	25 μM
Incubation Time:	24 hours
Result:	Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models.

Apoptosis Analysis

Cell Line:	LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells
Concentration:	0 μM, 10 μM, 25 μM, 50 μM
Incubation Time:	24 hours
Result:	Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma in all PCa cells.

Western Blot Analysis

Cell Line:	LNCaP and PC3 cells
Concentration:	0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM
Incubation Time:	30 minutes
Result:	Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed.

体内研究
(In Vivo)

MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth.

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

Animal Model:	C57 BL/6 male mice bearing LNCaP tumors
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; daily; for 14 days
Result:	Led to a 33% inhibition of tumor growth.

体内研究

MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth.

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

Animal Model:	C57 BL/6 male mice bearing LNCaP tumors
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; daily; for 14 days
Result:	Led to a 33% inhibition of tumor growth.

体内研究

MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth.

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

Animal Model:	C57 BL/6 male mice bearing LNCaP tumors
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; daily; for 14 days
Result:	Led to a 33% inhibition of tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (383.02 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0642 mL	15.3210 mL	30.6419 mL
5 mM	0.6128 mL	3.0642 mL	6.1284 mL
10 mM	0.3064 mL	1.5321 mL	3.0642 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。

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: ≥ 2.08 mg/mL (6.37 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.37 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.37 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.37 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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